Search Result

Pathways Recommended:	TGF-beta/Smad
Targets Recommended:	TGF-beta/Smad β-catenin GSK-3 TGF-β Receptor Beta-secretase Dopamine β-hydroxylase PI3K FLT3 Oct3/4 Arp2/3 Complex Na+/HCO3- Cotransporter MAP3K Ligand for E3 Ligase Indoleamine 2,3-Dioxygenase (IDO) E3 Ligase Ligand-Linker Conjugate Adrenergic Receptor Progesterone Receptor Amyloid-β E1/E2/E3 Enzyme IFNAR PIKfyve TAM Receptor Dopamine Transporter ATM/ATR

Results for "Active Integrinalpha 2b beta 3 Inhibitors" in MCE Product Catalog:

By Targets:	Adrenergic Receptor (30) Amyloid-β (12) Arp2/3 Complex (1) ATM/ATR (4) Beta-secretase (7) Dopamine Transporter (1) Dopamine β-hydroxylase (3) E1/E2/E3 Enzyme (6) FLT3 (11) GSK-3 (6) IFNAR (2) Indoleamine 2,3-Dioxygenase (IDO) (4) Ligand for E3 Ligase (3) MAP3K (2) PI3K (23) Progesterone Receptor (5) TAM Receptor (4) TGF-beta/Smad (1) TGF-β Receptor (7) β-catenin (1) 5 alpha Reductase (3) 5-HT Receptor (67) Acetyl-CoA Carboxylase (1) AChE (13) Acyltransferase (7) ADC Cytotoxin (4) Adenosine Receptor (16) Adenylate Cyclase (1) Adiponectin Receptor (3) Akt (13) Aldose Reductase (5) ALK (8) Aminopeptidase (1) AMPK (7) Androgen Receptor (11) Angiotensin Receptor (10) Angiotensin-converting Enzyme (ACE) (9) Antibiotic (70) Antifolate (6) Apoptosis (149) Arginase (3) Aromatase (1) Aryl Hydrocarbon Receptor (4) ATP Citrate Lyase (1) Aurora Kinase (3) Autophagy (101) Bacterial (150) Bcl-2 Family (9) Bcr-Abl (10) BCRP (1) BMX Kinase (1) Bradykinin Receptor (3) Btk (16) c-Fms (10) c-Kit (11) c-Met/HGFR (7) c-Myc (1) Calcium Channel (14) CaMK (2) Cannabinoid Receptor (9) Carbonic Anhydrase (1) Casein Kinase (4) Caspase (8) CaSR (6) Cathepsin (6) CCR (13) CDK (17) CFTR (3) CGRP Receptor (1) Checkpoint Kinase (Chk) (1) Chloride Channel (2) Cholecystokinin Receptor (8) CMV (3) Complement System (6) COMT (4) COX (23) CRM1 (1) CXCR (9) Cytochrome P450 (31) Deubiquitinase (1) Dihydroorotate Dehydrogenase (2) Dipeptidyl Peptidase (6) Discoidin Domain Receptor (1) DNA Alkylator/Crosslinker (3) DNA Methyltransferase (1) DNA-PK (1) DNA/RNA Synthesis (30) Dopamine Receptor (32) Drug Metabolite (57) Drug-Linker Conjugates for ADC (3) DYRK (2) EGFR (29) Elastase (1) Endogenous Metabolite (54) Endothelin Receptor (11) Enterovirus (2) Ephrin Receptor (2) Epigenetic Reader Domain (20) Epoxide Hydrolase (2) ERK (8) Estrogen Receptor/ERR (24) Eukaryotic Initiation Factor (eIF) (1) FAAH (1) Factor Xa (6) Farnesyl Transferase (2) Fatty Acid Synthase (FASN) (2) Ferroptosis (10) FGFR (6) Filovirus (3) FKBP (1) FLAP (5) Fungal (27) FXR (5) GABA Receptor (11) Galectin (2) Gap Junction Protein (1) GHSR (2) Glucagon Receptor (2) Glucocorticoid Receptor (12) Glucokinase (3) Glucosidase (3) GLUT (2) Glutaminase (2) Glutathione Peroxidase (2) GlyT (1) GNRH Receptor (2) GPR109A (2) GPR40 (3) GPR84 (3) Guanylate Cyclase (4) Gutathione S-transferase (4) HBV (12) HCV (28) HCV Protease (7) HDAC (11) Hedgehog (2) HIF/HIF Prolyl-Hydroxylase (16) Histamine Receptor (38) Histone Acetyltransferase (3) Histone Demethylase (10) Histone Methyltransferase (18) HIV (21) HIV Integrase (1) HIV Protease (3) HMG-CoA Reductase (HMGCR) (8) HSP (8) HSV (8) IAP (1) IGF-1R (5) iGluR (36) IKK (4) Imidazoline Receptor (1) Influenza Virus (24) Insulin Receptor (2) Integrin (8) Interleukin Related (7) IRAK (5) Isocitrate Dehydrogenase (IDH) (4) JAK (22) JNK (5) Keap1-Nrf2 (3) Lactate Dehydrogenase (3) Leukotriene Receptor (15) Ligand for Target Protein for PROTAC (1) LIM Kinase (LIMK) (1) Lipoxygenase (6) LPL Receptor (12) LRRK2 (2) LXR (2) mAChR (10) MAGL (3) MAP4K (2) MAPKAPK2 (MK2) (2) MCHR1 (GPR24) (2) MDM-2/p53 (9) MEK (6) Melanocortin Receptor (6) Melatonin Receptor (2) mGluR (7) MicroRNA (4) Microtubule/Tubulin (9) Mineralocorticoid Receptor (1) Mitochondrial Metabolism (3) Mitophagy (4) MMP (11) MNK (1) Monoamine Oxidase (12) Monoamine Transporter (1) Monocarboxylate Transporter (1) Motilin Receptor (1) mTOR (5) Na+/K+ ATPase (2) nAChR (6) NADPH Oxidase (2) Nampt (4) NEDD8-activating Enzyme (2) Neprilysin (6) Neurokinin Receptor (6) Neuropeptide Y Receptor (3) Neurotensin Receptor (2) NF-κB (22) NO Synthase (12) NOD-like Receptor (NLR) (2) Notch (3) Nucleoside Antimetabolite/Analog (12) Opioid Receptor (11) Orexin Receptor (OX Receptor) (6) P-glycoprotein (4) P2X Receptor (6) P2Y Receptor (5) p38 MAPK (27) Parasite (37) PARP (10) PD-1/PD-L1 (3) PDGFR (12) PDHK (2) PERK (3) PGE synthase (5) Phosphatase (10) Phosphodiesterase (PDE) (26) Phospholipase (5) PI4K (3) Pim (2) PKA (3) PKC (7) Potassium Channel (22) PPAR (11) Prostaglandin Receptor (20) PROTAC (1) PROTAC Linker (10) Protease-Activated Receptor (PAR) (4) Proteasome (4) Protein Arginine Deiminase (3) Proton Pump (7) Raf (4) RAR/RXR (2) Ras (11) Reactive Oxygen Species (18) Renin (1) RET (1) Reverse Transcriptase (5) Ribosomal S6 Kinase (RSK) (2) RIP kinase (3) ROCK (5) ROR (8) ROS (4) RSV (3) Salt-inducible Kinase (SIK) (1) SARS-CoV (13) Ser/Thr Protease (2) Serotonin Transporter (5) SGK (1) SGLT (7) Sigma Receptor (3) Sirtuin (7) Smo (2) Sodium Channel (14) Somatostatin Receptor (2) SPHK (3) Src (13) STAT (7) Syk (11) Thrombin (10) Thrombopoietin Receptor (1) Thymidylate Synthase (2) Thyroid Hormone Receptor (7) TNF Receptor (10) Toll-like Receptor (TLR) (7) TOPK (2) Topoisomerase (9) Trk Receptor (3) TRP Channel (13) Tyrosinase (1) ULK (1) Vasopressin Receptor (3) VD/VDR (14) VEGFR (17) Virus Protease (8) Wnt (3) Xanthine Oxidase (2) γ-secretase (7)
By Research Areas:	Cancer (702) Cardiovascular Disease (173) Endocrinology (156) Infection (286) Inflammation/Immunology (469) Metabolic Disease (229) Neurological Disease (408)

By Targets:

Adrenergic Receptor (30)

Amyloid-β (12)

Arp2/3 Complex (1)

ATM/ATR (4)

Beta-secretase (7)

Dopamine Transporter (1)

Dopamine β-hydroxylase (3)

E1/E2/E3 Enzyme (6)

FLT3 (11)

GSK-3 (6)

IFNAR (2)

Indoleamine 2,3-Dioxygenase (IDO) (4)

Ligand for E3 Ligase (3)

MAP3K (2)

PI3K (23)

Progesterone Receptor (5)

TAM Receptor (4)

TGF-beta/Smad (1)

TGF-β Receptor (7)

β-catenin (1)

5 alpha Reductase (3)

5-HT Receptor (67)

Acetyl-CoA Carboxylase (1)

AChE (13)

Acyltransferase (7)

ADC Cytotoxin (4)

Adenosine Receptor (16)

Adenylate Cyclase (1)

Adiponectin Receptor (3)

Akt (13)

Aldose Reductase (5)

ALK (8)

Aminopeptidase (1)

AMPK (7)

Androgen Receptor (11)

Angiotensin Receptor (10)

Angiotensin-converting Enzyme (ACE) (9)

Antibiotic (70)

Antifolate (6)

Apoptosis (149)

Arginase (3)

Aromatase (1)

Aryl Hydrocarbon Receptor (4)

ATP Citrate Lyase (1)

Aurora Kinase (3)

Autophagy (101)

Bacterial (150)

Bcl-2 Family (9)

Bcr-Abl (10)

BCRP (1)

BMX Kinase (1)

Bradykinin Receptor (3)

Btk (16)

c-Fms (10)

c-Kit (11)

c-Met/HGFR (7)

c-Myc (1)

Calcium Channel (14)

CaMK (2)

Cannabinoid Receptor (9)

Carbonic Anhydrase (1)

Casein Kinase (4)

Caspase (8)

CaSR (6)

Cathepsin (6)

CCR (13)

CDK (17)

CFTR (3)

CGRP Receptor (1)

Checkpoint Kinase (Chk) (1)

Chloride Channel (2)

Cholecystokinin Receptor (8)

CMV (3)

Complement System (6)

COMT (4)

COX (23)

CRM1 (1)

CXCR (9)

Cytochrome P450 (31)

Deubiquitinase (1)

Dihydroorotate Dehydrogenase (2)

Dipeptidyl Peptidase (6)

Discoidin Domain Receptor (1)

DNA Alkylator/Crosslinker (3)

DNA Methyltransferase (1)

DNA-PK (1)

DNA/RNA Synthesis (30)

Dopamine Receptor (32)

Drug Metabolite (57)

Drug-Linker Conjugates for ADC (3)

DYRK (2)

EGFR (29)

Elastase (1)

Endogenous Metabolite (54)

Endothelin Receptor (11)

Enterovirus (2)

Ephrin Receptor (2)

Epigenetic Reader Domain (20)

Epoxide Hydrolase (2)

ERK (8)

Estrogen Receptor/ERR (24)

Eukaryotic Initiation Factor (eIF) (1)

FAAH (1)

Factor Xa (6)

Farnesyl Transferase (2)

Fatty Acid Synthase (FASN) (2)

Ferroptosis (10)

FGFR (6)

Filovirus (3)

FKBP (1)

FLAP (5)

Fungal (27)

FXR (5)

GABA Receptor (11)

Galectin (2)

Gap Junction Protein (1)

GHSR (2)

Glucagon Receptor (2)

Glucocorticoid Receptor (12)

Glucokinase (3)

Glucosidase (3)

GLUT (2)

Glutaminase (2)

Glutathione Peroxidase (2)

GlyT (1)

GNRH Receptor (2)

GPR109A (2)

GPR40 (3)

GPR84 (3)

Guanylate Cyclase (4)

Gutathione S-transferase (4)

HBV (12)

HCV (28)

HCV Protease (7)

HDAC (11)

Hedgehog (2)

HIF/HIF Prolyl-Hydroxylase (16)

Histamine Receptor (38)

Histone Acetyltransferase (3)

Histone Demethylase (10)

Histone Methyltransferase (18)

HIV (21)

HIV Integrase (1)

HIV Protease (3)

HMG-CoA Reductase (HMGCR) (8)

HSP (8)

HSV (8)

IAP (1)

IGF-1R (5)

iGluR (36)

IKK (4)

Imidazoline Receptor (1)

Influenza Virus (24)

Insulin Receptor (2)

Integrin (8)

Interleukin Related (7)

IRAK (5)

Isocitrate Dehydrogenase (IDH) (4)

JAK (22)

JNK (5)

Keap1-Nrf2 (3)

Lactate Dehydrogenase (3)

Leukotriene Receptor (15)

Ligand for Target Protein for PROTAC (1)

LIM Kinase (LIMK) (1)

Lipoxygenase (6)

LPL Receptor (12)

LRRK2 (2)

LXR (2)

mAChR (10)

MAGL (3)

MAP4K (2)

MAPKAPK2 (MK2) (2)

MCHR1 (GPR24) (2)

MDM-2/p53 (9)

MEK (6)

Melanocortin Receptor (6)

Melatonin Receptor (2)

mGluR (7)

MicroRNA (4)

Microtubule/Tubulin (9)

Mineralocorticoid Receptor (1)

Mitochondrial Metabolism (3)

Mitophagy (4)

MMP (11)

MNK (1)

Monoamine Oxidase (12)

Monoamine Transporter (1)

Monocarboxylate Transporter (1)

Motilin Receptor (1)

mTOR (5)

Na+/K+ ATPase (2)

nAChR (6)

NADPH Oxidase (2)

Nampt (4)

NEDD8-activating Enzyme (2)

Neprilysin (6)

Neurokinin Receptor (6)

Neuropeptide Y Receptor (3)

Neurotensin Receptor (2)

NF-κB (22)

NO Synthase (12)

NOD-like Receptor (NLR) (2)

Notch (3)

Nucleoside Antimetabolite/Analog (12)

Opioid Receptor (11)

Orexin Receptor (OX Receptor) (6)

P-glycoprotein (4)

P2X Receptor (6)

P2Y Receptor (5)

p38 MAPK (27)

Parasite (37)

PARP (10)

PD-1/PD-L1 (3)

PDGFR (12)

PDHK (2)

PERK (3)

PGE synthase (5)

Phosphatase (10)

Phosphodiesterase (PDE) (26)

Phospholipase (5)

PI4K (3)

Pim (2)

PKA (3)

PKC (7)

Potassium Channel (22)

PPAR (11)

Prostaglandin Receptor (20)

PROTAC (1)

PROTAC Linker (10)

Protease-Activated Receptor (PAR) (4)

Proteasome (4)

Protein Arginine Deiminase (3)

Proton Pump (7)

Raf (4)

RAR/RXR (2)

Ras (11)

Reactive Oxygen Species (18)

Renin (1)

RET (1)

Reverse Transcriptase (5)

Ribosomal S6 Kinase (RSK) (2)

RIP kinase (3)

ROCK (5)

ROR (8)

ROS (4)

RSV (3)

Salt-inducible Kinase (SIK) (1)

SARS-CoV (13)

Ser/Thr Protease (2)

Serotonin Transporter (5)

SGK (1)

SGLT (7)

Sigma Receptor (3)

Sirtuin (7)

Smo (2)

Sodium Channel (14)

Somatostatin Receptor (2)

SPHK (3)

Src (13)

STAT (7)

Syk (11)

Thrombin (10)

Thrombopoietin Receptor (1)

Thymidylate Synthase (2)

Thyroid Hormone Receptor (7)

TNF Receptor (10)

Toll-like Receptor (TLR) (7)

TOPK (2)

Topoisomerase (9)

Trk Receptor (3)

TRP Channel (13)

Tyrosinase (1)

ULK (1)

Vasopressin Receptor (3)

VD/VDR (14)

VEGFR (17)

Virus Protease (8)

Wnt (3)

Xanthine Oxidase (2)

γ-secretase (7)

By Research Areas:

Cancer (702)

Cardiovascular Disease (173)

Endocrinology (156)

Infection (286)

Inflammation/Immunology (469)

Metabolic Disease (229)

Neurological Disease (408)

2030

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

Peptides

309

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-P1114

2B-(SP)
GSK-3 Neurological Disease

2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3.
HY-P1114A

2B-(SP) (TFA)
GSK-3 Cancer

2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3.

2B-(SP)	GSK-3	Neurological Disease
2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3.

2B-(SP) (TFA)	GSK-3	Cancer
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3.

HY-U00321

A2B receptor antagonist 1	Adenosine Receptor	Inflammation/Immunology Cancer
A2B receptor antagonist 1 is a potent A2B adenosine receptor antagonist extracted from patent WO 2009157938 A1 EXAMPLE 9B.

HY-P0117

Tat-NR2B9c Tat-NR2bct; NA-1	iGluR NO Synthase	Neurological Disease
Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

HY-B1915

Micronomicin Gentamicin C2b; Antibiotic XK-62-2; Sagamicin	Bacterial	Infection
Micronomicin (Gentamicin C2b) is an aminoglycoside antibiotic, with antibacterial and bactericidal activities.

HY-P0117A

Tat-NR2B9c TFA Tat-NR2bct TFA; NA-1 TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

HY-125021

2BAct	Eukaryotic Initiation Factor (eIF)	Neurological Disease
2BAct is a highly selective, CNS-permeable, and orally active *eIF2B* (eukaryotic initiation factor 2B) activator with an EC₅₀ of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response.

HY-12294

PEAQX NVP-AAM077	iGluR	Neurological Disease
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).

HY-12294A

PEAQX tetrasodium hydrate NVP-AAM077 tetrasodium hydrate	iGluR Apoptosis	Neurological Disease
PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).

HY-103154

SB228357	5-HT Receptor	Neurological Disease
SB228357 is a selective, potent and orall active 5-HT_2C/2B receptor antagonist with pK_i values of 6.9, 8.0 and 9.0 for *5-HT_2A, 5-HT_2B* and *5-HT_2C, respectively. SB228357 has antidepressant/anxiolytic effects.*

HY-B2006

Fenvalerate	Phosphatase Bacterial	Infection
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC₅₀ of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.

HY-106441A

Rislenemdaz MK-0657; CERC-301	iGluR	Neurological Disease
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with K_i and IC₅₀ of 8.1 nM and 3.6 nM, respectively.

HY-108307

Micronomicin sulfate Gentamicin C2b sulfate; Antibiotic XK-62-2 sulfate; Sagamicin sulfate	Antibiotic Bacterial	Infection
Micronomicin sulfate (Gentamicin C2b sulfate) is an aminoglycoside antibiotic isolated from Micromonospora. Micronomicin sulfate is a broad-spectrum antibiotic close to the gentamicin-type antibiotics, exhibits a high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc (MIC=0.001-8.3 μg/ml).

HY-15472

PRX-08066	5-HT Receptor	Cardiovascular Disease
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

HY-11100

Asenapine maleate Org 5222 maleate	5-HT Receptor	Neurological Disease
Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with K_i values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.

HY-10121

Asenapine Org 5222	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.

HY-135785

OSMI-3	Acyltransferase	Metabolic Disease
OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.

HY-16567

Asenapine hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and *Dopamine (D₂,* D₃, D₄) receptor antagonist with K_i** values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.

HY-116463C

*(2R,3R)-E1R*	Sigma Receptor	Neurological Disease
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.

HY-126057S

(R)-Praziquantel D11	Parasite 5-HT Receptor	Infection
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.

HY-10238

Danoprevir ITMN-191; R7227; RO5190591; RG7227	HCV Protease HCV	Infection
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC₅₀ of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC₅₀ higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC₅₀s=0.2-0.4 nM) as well as 2b and 3a (IC₅₀s=1.6, 3.5 nM).

HY-103129

SB-200646A	5-HT Receptor	Neurological Disease
SB-200646A is the first selective *5-HT_2B/2C* over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for *5-HT_2B, 5-HT_2C* and 5-HT_2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

HY-103129A

SB-200646	5-HT Receptor	Neurological Disease
SB-200646 is the first selective *5-HT_2B/2C* over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for *5-HT_2B, 5-HT_2C* and 5-HT_2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.

HY-114204

GSK8814	Epigenetic Reader Domain	Cancer
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pK_d=8.1 and a pK_i=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC₅₀s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.

HY-P2307

Tat-NR2Baa	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.

HY-P2307A

Tat-NR2Baa TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.

HY-N7136

α-Terpinyl acetate	Cytochrome P450	Metabolic Disease
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a K_d value of 5.4 μM.

HY-N3513

Mulberrin Kuwanon C	Others	Cardiovascular Disease
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC₅₀ value being 1.8 ±1.5 μM.

HY-100014

KDM5A-IN-1	Histone Demethylase	Cancer
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC₅₀ value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).

HY-18596

SB-215505	5-HT Receptor	Neurological Disease
SB-215505 is a potent and subtype-selective *5-HT_2B* receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively. SB-215505 increases wakefulness and motor activity in rats.

HY-100637

Hydroxybupropion	Adrenergic Receptor nAChR	Neurological Disease
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC₅₀ value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonis tis more potent than Bupropion .

HY-13993

Ro 25-6981	iGluR	Neurological Disease
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.

HY-111767

BAY-545	Adenosine Receptor	Inflammation/Immunology
BAY-545 is a potent and selective A_2B adenosine receptor antagonist, with an IC₅₀ of 59 nM. BAY-545 also exhibits IC₅₀s of 66, 400, 280 nM for human, mouse, rat A_2B adenosine receptor in cells, respectively, and a K_i of 97 nM for human A_2B adenosine receptor, with more selectivity over A₁, A_2A, and A₃ adenosine receptor.

HY-108539

CE3F4	Others	Metabolic Disease
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC₅₀s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

HY-15419

RS-127445 hydrochloride	5-HT Receptor	Neurological Disease
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5 and 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-136299

Sepimostat FUT-187 free base	iGluR	Neurological Disease
Sepimostat exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a K_i value of 27.7 µM.

HY-15419A

RS-127445	5-HT Receptor	Neurological Disease
RS-127445 is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5 and 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-N5132

(-)-Fenchone	Others	Others
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Thuja occidentalis. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6.

HY-14390

LAS101057
Adenosine Receptor Inflammation/Immunology

LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.

LAS101057	Adenosine Receptor	Inflammation/Immunology
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.

HY-15296

Cabergoline FCE-21336	Dopamine Receptor Autophagy	Endocrinology
Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and *5-HT_2B* receptors (K_i=0.7, 1.5, and 1.2, respectively).

HY-103186

MRS-1706	Adenosine Receptor	Inflammation/Immunology
MRS-1706 is a potent and selective *adenosine A_2B* receptor inverse agonist. MRS-1706 has K_i** values of 1.39, 112, 157, and 230 nM for human A_2B, A_2A, A₁ and A₃ receptors respectively.

HY-13409A

SB 242084 hydrochloride	5-HT Receptor	Neurological Disease
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.

HY-13409

SB 242084	5-HT Receptor	Neurological Disease
SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.

HY-N0859

Schisanhenol
Schizanhenol; Gomisin-K3
Others Cancer

Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
HY-B0531

Triflusal
COX Inflammation/Immunology

Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.

Schisanhenol Schizanhenol; Gomisin-K3	Others	Cancer
Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.

Triflusal	COX	Inflammation/Immunology
Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.

HY-14777

Radiprodil RGH-896	iGluR	Neurological Disease
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.

HY-12451

FICZ
6-Formylindolo[3,2-b]carbazole
Aryl Hydrocarbon Receptor Others

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a K_d of 70 pM.
HY-B1184

Mephenytoin
Cytochrome P450 Neurological Disease

Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.

FICZ 6-Formylindolo[3,2-b]carbazole	Aryl Hydrocarbon Receptor	Others
FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a K_d of 70 pM.

HY-12962

NMDA-IN-1	iGluR	Neurological Disease
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.

HY-13993A

Ro 25-6981 Maleate
iGluR Neurological Disease

Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.

HY-110279

Ogerin	Others	Neurological Disease
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC₅₀ of 6.83. Ogerin shows inverse agonist and antagonist activity (K_i, 220 nM) at A_2A receptoor and weak antagonist activity (K_i, 736 nM) at 5-HT_2B receptor. Ogerin blocks recall in fear conditioning in mice.

HY-19764

*GSK2983559 active* metabolite**	RIP kinase	Cancer
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

HY-107774

BMS-986163	iGluR	Neurological Disease
BMS-986163 is a negative allosteric modulator of *GluN2B. The prodrug BMS-986163 rapidly converts to its active* parent molecule BMS-986169 (K_i=4 nM, IC₅₀=24 nM).

HY-10559

Nelotanserin APD125	5-HT Receptor	Cancer Neurological Disease
Nelotanserin is a potent *5-HT_2A* inverse agonist, a moderately potent *5-HT_2C* partial inverse agonist and a weak *5-HT_2B* inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

HY-111500A

NMDAR antagonist 1
iGluR Neurological Disease

NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.

HY-15543A

CP-809101 hydrochloride	5-HT Receptor	Neurological Disease
CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.

HY-15543

CP-809101	5-HT Receptor	Neurological Disease
CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.

HY-136459

NMDA receptor antagonist 2	iGluR	Neurological Disease
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC₅₀ and a K_i of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.

HY-118152

Org-12962	5-HT Receptor	Neurological Disease
Org-12962 is a potent, selective and orally active *5-HT_2C receptor* agonist with a pEC₅₀ value of 7.01. Org-12962 also exhibits high effacy for the 5-HT_2A and 5-HT_2B receptor with pEC₅₀s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.

HY-106136

TIK-301 PD-6735; LY-156735	Melatonin Receptor 5-HT Receptor	Neurological Disease
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT_2B/5-HT_2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

HY-15658

GSK2801	Epigenetic Reader Domain	Cancer
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive *BAZ2A* and *BAZ2B* bromodomains inhibitor with K_d values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for *BAZ2A/B* over BRD4.

HY-103110A

ST1936 oxalate	5-HT Receptor	Neurological Disease
ST1936 oxalate is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.

HY-14121

MRS 1754	Adenosine Receptor	Metabolic Disease Inflammation/Immunology
MRS 1754 is a selective antagonist radioligand for A_2B adenosine receptor with very low affinity for A₁ and A₃ receptors of both humans and rats.

HY-U00439

Protein kinase inhibitors 1
DYRK Cancer

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.

HY-103138A

(Rac)-WAY-161503	5-HT Receptor	Metabolic Disease Neurological Disease
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT_2C receptor agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.

HY-19306

SB-267268	Integrin	Cancer
SB-267268 is a selective and nonpeptidic **alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with K_is of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC₅₀**s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.

HY-111500

(Rac)-NMDAR antagonist 1	iGluR	Neurological Disease
(Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.

HY-17416

Guanfacine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.

HY-B0365A

Memantine hydrochloride D-145 hydrochloride	Cytochrome P450 iGluR Autophagy	Neurological Disease
Memantine (hydrochloride) (D-145 (hydrochloride)), an amantadine derivative with low to moderate-affinity for NMDA receptors, inhibit CYP2B6 and CYP2D6 with K_i of 0.51 nM and 94.9 μM, respectively.

HY-10081

GS-6201 CVT-6883	Adenosine Receptor	Inflammation/Immunology
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (K_i=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.

HY-B0822

Fipronil	GABA Receptor Cytochrome P450	Neurological Disease
Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC₅₀s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC₅₀0s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms *CYP1A1/2, CYP2B1/2, and CYP3A1/2* in isolated rat liver microsomes.

HY-100300

AGN 192836	Adrenergic Receptor	Cardiovascular Disease Endocrinology
AGN 192836 is a potent and selective α2 adrenergic agonist with EC₅₀s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

HY-140513

Active-mono-sulfone-PEG8-acid
PROTAC Linker Cancer

Active-mono-sulfone-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-12882A

Ifenprodil tartrate	iGluR Potassium Channel	Neurological Disease
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.

HY-U00244

Benzquinamide P2647; BZQ; Benzoquinamide	Adrenergic Receptor	Metabolic Disease Endocrinology
Benzquinamide (P2647) is an antiemetic which can bind to the *α_2A, α_2B, and α_2C* adrenergic receptors (α2-AR) with K_i values of 1,365, 691, and 545 nM, respectively.

HY-101610

OPC-28326	Adrenergic Receptor	Cardiovascular Disease Endocrinology
OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with K_i of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.

HY-111490

Desisobutyryl-ciclesonide CIC-AP; Ciclesonide Active principle	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.

HY-14873

Tonapofylline BG 9928	Adenosine Receptor	Metabolic Disease Cardiovascular Disease
Tonapofylline (BG 9928) is an orally active and selective adenosine A₁ receptor antagonist with a K_i of 7.4 nM for human adenosine A₁ receptor (hA₁), which displays 915-fold selectivity versus human adenosine A_2A receptor and 12-fold selectivity versus human adenosine A_2B receptor and is used in development for the treatment of heart failure.

HY-100029B

*Bay 41-4109 (less active* enantiomer)**	HBV	Infection
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC₅₀ of 53 nM.

HY-109112

Brilaroxazine RP5063	Dopamine Receptor 5-HT Receptor	Inflammation/Immunology Neurological Disease
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

HY-10895

SB-334867 SB 334867A	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over *OX2* (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

HY-P0162

HCV-IN-4	HCV	Infection
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC₉₀s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively.

HY-112254

ZINC03129319	Virus Protease	Infection
ZINC03129319 is a dengue virus (DENV) NS2B-NS3 protease inhibitor extracted from patent US20150141521A1, has inhibition constants (K_i1) of 92 μM and *K_i3* of 20 μM.

HY-B1101

Pimethixene Pimetixene	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-10895A

SB-334867 free base SB334867A free base	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over *OX2* (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

HY-B1101A

Pimethixene maleate Pimetixene maleate	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-100678

CGS 15943	Adenosine Receptor PI3K	Cancer Inflammation/Immunology
CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its K_i for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. ^[1].

HY-12881

Eliprodil SL-820715	iGluR	Neurological Disease
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).

HY-105285

Piromelatine Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

HY-106408A

Salfaprodil Neu2000 potassium	iGluR	Neurological Disease
Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death.

HY-N3522

Platycoside E	Others	Inflammation/Immunology
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific *IgG2a* and *IgG2b* antibody in the ovalbumin (OVA)-immunized mice.

HY-108323

CCR2 antagonist 4 Teijin compound 1	CCR	Inflammation/Immunology
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific *CCR2* antagonist, with IC₅₀s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC₅₀ of 24 nM.

HY-103362

CCR2 antagonist 4 hydrochloride Teijin compound 1 hydrochloride	CCR	Inflammation/Immunology
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific *CCR2* antagonist, with IC₅₀s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC₅₀ of 24 nM.

HY-19533

SCH 58261	Adenosine Receptor	Cancer
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC₅₀ of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.

HY-135331

N-Desmethyl Apalutamide	Androgen Receptor Cytochrome P450	Cancer
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong *CYP3A4* and *CYP2B6* inducer and has an excellent plasma-proteins bound concentration.

HY-N2071

Cedrol (+)-Cedrol; α-Cedrol	Cytochrome P450 Fungal	Infection Inflammation/Immunology Cancer
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.

HY-106408

Salfaprodil free base Neu2000	iGluR	Neurological Disease
Salfaprodil free base (Neu2000) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil free base has excellent neuroprotection against NMDA- and free radical-induced cell death.

HY-B0371D

(S)-Terazosin	Adrenergic Receptor	Endocrinology
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with K_i values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for *α2a, α2B* and *α2c*-adrenoceptor with K_i values of 729 nM, 3.5 nM and 46.4 nM, respectively.

HY-13953

JIB-04	Histone Demethylase Apoptosis	Cancer
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC₅₀s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.

HY-N0049

Nuciferine	5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), *5-HT_2C* (IC₅₀=131 nM), and *5-HT_2B* (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-15703

QNZ46	iGluR	Neurological Disease
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).

HY-A0007

Rotigotine Hydrochloride N-0923 Hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-P1115

AKTide-2T	Akt	Others
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.

HY-P1115A

AKTide-2T TFA	Akt	Others
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.

HY-15298C

Grazoprevir sodium salt MK-5172 (sodium salt)	HCV HCV Protease	Infection
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-15298B

Grazoprevir hydrate MK-5172 (hydrate)	HCV HCV Protease
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-75502

Rotigotine N-0437; N-0923	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-15298

Grazoprevir MK-5172	HCV Protease HCV	Infection
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-15298A

Grazoprevir potassium salt MK-5172 (potassium salt)	HCV HCV Protease	Infection
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-15394

(Rac)-Rotigotine hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Endocrinology Neurological Disease
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-136573

5-Hydroxytoluene-2,4-disulphonic acid diammonium	Virus Protease	Infection
5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC₅₀ of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC₅₀ of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.

HY-136575

4-Hydroxy-2-methylbenzenesulfonic acid ammonium	Virus Protease	Infection
4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC₅₀ of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC₅₀ of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.

HY-103171

BAY 60-6583	Adenosine Receptor	Inflammation/Immunology Cardiovascular Disease
BAY 60-6583 is a potent and high-affinity agonist of adenosine A_2B receptor (EC₅₀ = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with K_i values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.

HY-136574

2-Hydroxy-4-methylbenzenesulphonic acid ammonium	Virus Protease	Infection
2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC₅₀ of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC₅₀ of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.

HY-17356

Fenofibrate	PPAR Cytochrome P450 Autophagy	Cardiovascular Disease Cancer
Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for *CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4*, respectively.

HY-N6696

Aflatoxin B2	Bacterial Antibiotic	Cancer Infection
Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.

HY-N6698

Aflatoxin G2	Bacterial Antibiotic	Cancer Infection
Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.

HY-P2290

Beta-defensin 1, pig	Bacterial	Infection Inflammation/Immunology
Beta-defensin 1, pig is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig is active against bacteria such as *Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis* and Candida albicans.

HY-B1837A

β-Cyfluthrin beta-Cyfluthrin	Calcium Channel	Infection
β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca²⁺ ATPase involved in calcium transport.

HY-N6700

Aflatoxin M2	Others	Cancer
Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.

HY-108573

P-1075	Potassium Channel	Cardiovascular Disease
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-K_IR6), with an EC₅₀ value of 45 nM for SUR2B-K_IR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.

HY-N6699

Aflatoxin M1	Bacterial	Cancer Infection
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.

HY-N4180

*Pennogenin 3-O-beta-chacotrioside*	Autophagy	Cancer
Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.

HY-12177S

Aliskiren D6 hemifumarate CGP 60536 D6 hemifumarate; CGP60536B D6 hemifumarate; SPP 100 D6 hemifumarate	Renin Autophagy	Cancer Cardiovascular Disease
Aliskiren D6 hemifumarate (CGP 60536 D6 hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC₅₀ of 1.5 nM.

HY-P2290A

Beta-defensin 1, pig TFA	Bacterial	Infection Inflammation/Immunology
Beta-defensin 1, pig TFA is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig TFA is active against bacteria such as *Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis* and Candida albicans.

HY-101918

DS-1040 Tosylate	Others	Cardiovascular Disease
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC₅₀s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

HY-B1800

Tolonidine	Others	Cardiovascular Disease
Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties.

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-10256A

SB 203580 hydrochloride RWJ 64809 hydrochloride	p38 MAPK Autophagy Mitophagy	Inflammation/Immunology Cancer
SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for *SAPK2a/p38* and *SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy* and mitophagy activator.

HY-100656

Desmethyl cariprazine	Dopamine Receptor 5-HT Receptor Drug Metabolite	Neurological Disease
Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (K_i=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).

HY-12222

Obeticholic acid INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid	FXR Autophagy	Others
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC₅₀ of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces *autophagy*.

HY-129491

O-Desmethyl Midostaurin CGP62221; O-Desmethyl PKC412	PKC	Cancer
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor with IC₅₀ ranging from 22-500 nM.

HY-15284

Prasugrel PCR 4099	P2Y Receptor	Cardiovascular Disease
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent *P2Y12* receptor antagonist, and inhibits ADP-induced platelet aggregation.

HY-15284A

Prasugrel hydrochloride PCR 4099 hydrochloride	P2Y Receptor	Cardiovascular Disease
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent *P2Y12* receptor antagonist, and inhibits ADP-induced platelet aggregation.

HY-10256

SB 203580 RWJ 64809	p38 MAPK Autophagy Mitophagy	Inflammation/Immunology Cancer
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for *SAPK2a/p38* and *SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy* and mitophagy activator.

HY-15284B

Prasugrel (Maleic acid) PCR 4099 (Maleic acid)	P2Y Receptor	Cardiovascular Disease
Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent *P2Y12* receptor antagonist, and inhibits ADP-induced platelet aggregation.

HY-100638

RPR132595A
NPC
Others Cancer

RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
HY-19522

Seladelpar
MBX-8025
PPAR Metabolic Disease

Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC₅₀ 2 nM), and specific PPAR-δ agonist.

HY-N7263

Galanthamine N-Oxide	AChE	Neurological Disease
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC₅₀ of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes.

HY-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

HY-N1501

Beta-asarone	Others	Inflammation/Immunology Neurological Disease
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.

HY-N2188

Beta-Acetoxyisovalerylshikonin
Others Inflammation/Immunology

Beta-Acetoxyisovalerylshikonin is a naphthoquinone derivative isolated from Arnebia euchroma.

HY-N6018

Beta-Eudesmol	TRP Channel	Metabolic Disease
Beta-Eudesmol is a natural oxygenated sesquiterpene, activates hTRPA1, with an EC₅₀ of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1.

HY-113418

Beta-Cortol
Endogenous Metabolite Endocrinology

Beta-Cortol is an androgen metabolite present in adults.

HY-N6740

Beta-Zearalanol	Apoptosis	Metabolic Disease
Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.

HY-136425

Fosetyl-aluminum Fosetyl-Al	Fungal	Infection
Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops.

HY-136300

PHD-1-IN-1	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology Cardiovascular Disease
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC₅₀ of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe²⁺ ion and induces the formation of an “Arg367-out” pocket.

HY-17642

Omidenepag	Prostaglandin Receptor	Endocrinology
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid *EP2* receptor agonist, with an EC₅₀ of 1.1 nM. Omidenepag shows binding affinities (IC₅₀) 10 nM for h-EP2.

HY-19373

RWJ-445167 3DP-10017	Thrombin Factor Xa	Cardiovascular Disease
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with K_i of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.

HY-16787

ICA-121431	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 µM).

HY-113974

trans-AUCB t-AUCB	Epoxide Hydrolase	Cancer
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC₅₀s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.

HY-N1484

7beta-Hydroxylathyrol
Others Others

7beta-Hydroxylathyrol is a natural product.

HY-100399

Nevanimibe PD-132301; ATR-101	Acyltransferase Apoptosis	Cancer
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC₅₀ of 9 nM. Nevanimibe inhibits ACAT2 with an EC₅₀ of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.

HY-100399A

Nevanimibe hydrochloride PD-132301 hydrochloride; ATR101 hydrochloride	Acyltransferase Apoptosis	Cancer
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC₅₀ of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC₅₀ of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.

HY-12047

Ponatinib AP24534	Bcr-Abl PDGFR VEGFR FGFR Src Autophagy	Cancer
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, *VEGFR2, FGFR1, and Src*, respectively.

HY-112608

CHMFL-PI3KD-317	PI3K	Cancer
CHMFL-PI3KD-317 is a highly potent, selective and orally active *PI3Kδ* inhibitor, with an IC₅₀ of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC₅₀, 62.6 nM), PI3Kβ (IC₅₀, 284 nM), PI3Kγ (IC₅₀, 202.7 nM), PIK3C2A (IC₅₀, >10000 nM), PIK3C2B (IC₅₀, 882.3 nM), VPS34 (IC₅₀, 1801.7 nM), PI4KIIIA (IC₅₀, 574.1 nM) and PI4KIIIB (IC₅₀, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC₅₀ of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.

HY-10274

Dabigatran etexilate BIBR 1048	Others	Cardiovascular Disease
Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.

HY-U00439A

*Protein kinase inhibitors* 1 hydrochloride** (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride	DYRK	Cancer
Protein kinase inhibitors 1 hydrochloride is a potent *HIPK2* inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2.

HY-107836

Methiothepin mesylate Metitepine mesylate; Ro 8-6837 mesylate	5-HT Receptor	Neurological Disease
Methiothepin mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-10274A

Dabigatran etexilate mesylate BIBR 1048MS; Dabigatran etexilate methanesulfonate	Others	Cardiovascular Disease
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.

HY-111406

Omidenepag isopropyl	Prostaglandin Receptor	Inflammation/Immunology
Omidenepag isopropyl is a selective *EP2* receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug.

HY-12047S

Ponatinib D8 AP24534 D8	Bcr-Abl PDGFR VEGFR FGFR Src Autophagy	Cancer
Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, *VEGFR2, FGFR1, and Src*, respectively.

HY-P2291

Beta-defensin 103 isoform X1, pig	Bacterial	Inflammation/Immunology
Beta-defensin 103 isoform X1, pig is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens.

HY-W012037

8-Hydroxyquinoline hemisulfate 8-Quinolinol hemisulfate	Bacterial Antibiotic	Infection
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.

HY-N2109

Macranthoidin A	Others	Metabolic Disease
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.

HY-19773

beta-lactamase-IN-1	Bacterial	Cancer
beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.

HY-N0087

Gambogic Acid beta-Guttiferrin	Bcl-2 Family Autophagy	Cancer
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, *Bcl-2, Bcl-W, Bcl-B, Bfl-1* and Mcl-1 with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

HY-N0941

beta-Mangostin
β-Mangostin
Others Others

beta-Mangostin is a natural product.

HY-P2291A

Beta-defensin 103 isoform X1, pig TFA	Bacterial	Inflammation/Immunology
Beta-defensin 103 isoform X1, pig TFA is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens.

HY-14165

Veliflapon BAY X 1005; DG-031	FLAP Leukotriene Receptor	Inflammation/Immunology Cardiovascular Disease
Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

HY-101402

Cyclo(his-pro) Cyclo(histidyl-proline); Histidylproline diketopiperazine	NF-κB Endogenous Metabolite	Inflammation/Immunology Neurological Disease
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.

HY-N6979

Crustecdysone 20-Hydroxyecdysone	Caspase Autophagy Endogenous Metabolite	Cardiovascular Disease
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (α-Ecdysone; HY-N0179)

HY-10181B

Dasatinib monohydrate BMS-354825 monohydrate	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib monohydrate (BMS-354825 monohydrate) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_i values of 16 pM and 30 pM for Src and Bcr-Abl, respectively.

HY-10181A

Dasatinib hydrochloride BMS-354825 hydrochloride	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with K_i values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity.

HY-101402A

Cyclo(his-pro) TFA Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA	NF-κB Endogenous Metabolite	Inflammation/Immunology Neurological Disease
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.

HY-135813

LtaS-IN-1	Bacterial	Infection
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.

HY-125957

A-3 hydrochloride	PKA Casein Kinase CaMK PKC	Others
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (K_i=4.3 µM), casein kinase II (K_i=5.1 µM) and myosin light chain kinase (MLCK) (K_i=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with K_i values of 47 µM and 80 µM, respectively.

HY-B1599

Chloramphenicol palmitate	Bacterial	Infection
Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.

HY-N2100

*6'-O-beta-D-Glucosylgentiopicroside*	Others	Metabolic Disease
6'-O-beta-D-Glucosylgentiopicroside is a secoiridoid isolated from the roots of G. straminea. 6'-O-beta-D-Glucosylgentiopicroside strongly suppresses N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation.

HY-N3523

3-O-Beta-D-Glucopyranosylplatycodigenin	Others	Cancer
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC₅₀ of 13.36 μM.

HY-N0406

2"-O-beta-L-galactopyranosylorientin	Others	Metabolic Disease
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).

HY-N2075

3-Acetyl-beta-boswellic acid
Others Inflammation/Immunology

3-Acetyl-beta-boswellic acid is a boswellic acid isolated from Boswellia serrata gum resin.

HY-10583

Y-27632 dihydrochloride	ROCK Apoptosis	Cancer
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with K_is of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.

HY-18728

STF-31
GLUT Autophagy Cancer

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].

HY-N4099

*Luteolin-3-O-beta-D-glucuronide*	Others	Infection Inflammation/Immunology
Luteolin-3-O-beta-D-glucuronide is a luteolin glucosiduronic acid consisting of luteolin having a beta-D-glucosiduronic acid residue attached at the 3'-position.

HY-P1524

Beta-Amyloid(1-14),mouse,rat
Amyloid-β Neurological Disease

Beta-Amyloid(1-14),mouse,rat is a 1 to 14 fragment of Amyloid-β peptide.

HY-125033

Beta-d-N4-hydroxycytidine NHC	Influenza Virus	Infection
Beta-d-N4-hydroxycytidine (NHC) is a very potent anti-VEEV (venezuelan equine encephalitis virus) agent with EC₅₀, EC₉₀, and EC₉₉ are 0.426, 1.036, and 2.5 μM, respectively.

HY-141131

Propargyl-PEG2-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG2-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141132

Propargyl-PEG4-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG4-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-N0411

β-Carotene Provitamin A; beta-Carotene	Endogenous Metabolite	Metabolic Disease
β-Carotene (Provitamin A) is an organic compound and classified as a terpenoid. It is a precursor (inactive form) of vitamin A.

HY-N2337

11beta-Hydroxyprogesterone 11β-Hydroxyprogesterone	Endogenous Metabolite	Cardiovascular Disease
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED₅₀ of 10 nM.

HY-140012

Azido-PEG4-beta-D-glucose
PROTAC Linker Cancer

Azido-PEG4-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-N2142

3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B	Others	Cancer
3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B is a chemical constituent of the plant Poria cocos .

HY-10181

Dasatinib BMS-354825	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC₅₀s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-Kit^D816V with IC₅₀s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment.

HY-15583

Auristatin F	Microtubule/Tubulin ADC Cytotoxin	Cancer
Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).

HY-N6260

4-O-beta-Glucopyranosyl-cis-coumaric acid
Others Others

4-O-beta-Glucopyranosyl-cis-coumaric acid is a natural compound isolated formn Nelumbo nucifera Gaertn.

HY-N2190

*Hederagenin 28-O-beta-D-glucopyranosyl ester*	Others	Inflammation/Immunology Cardiovascular Disease
Hederagenin 28-O-beta-D-glucopyranosyl ester, a triterpenoid saponin isolated from Ilex cornuta, exhibits protective effects against H₂O₂-induced myocardial cell injury.

HY-111642

3'-Azido-3'-deoxy-beta-L-uridine
Nucleoside Antimetabolite/Analog Others

3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.

HY-19974

TAK-220	CCR HIV	Infection Endocrinology
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC₅₀s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC₅₀s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC₉₀s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.

HY-122470

Stampidine	Reverse Transcriptase HIV	Infection
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV_IIIB (B-envelope subtype) and primary clinical isolates with IC₅₀s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC₅₀s of 8.7 nM and 11.2 nM, respectively.

HY-P1521

β-Amyloid 15-21
beta-Amyloid (15-21)
Amyloid-β Neurological Disease

β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
HY-141133

Propargyl-PEG4-tetra-Ac-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG4-tetra-Ac-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141135

Propargyl-PEG4-tetra-Ac-beta-D-galactose
PROTAC Linker Cancer

Propargyl-PEG4-tetra-Ac-beta-D-galactose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-15679

PI4KIII beta inhibitor 3
PI4K Cancer

PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC₅₀ of 5.7 nM.
HY-141127

Azido-PEG4-tetra-Ac-beta-D-glucose
PROTAC Linker Cancer

Azido-PEG4-tetra-Ac-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-125773

β-cyano-L-Alanine beta-cyano-l-alanine	Others	Neurological Disease
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.

HY-11007

GNF-2
Bcr-Abl SARS-CoV Cancer

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .
HY-N5039

1,2-O-Dilinoleoyl-3-O-Beta-D-Galactopyranosylracglycerol
Others Others

1,2-O-Dilinoleoyl-3-O-Beta-D-Galactopyranosylracglycerol is isolated from the flower of Magnolia denudate.
HY-P1522

β-Amyloid 29-40
Amyloid beta-protein(29-40)
Amyloid-β Neurological Disease

β-Amyloid (29-40) is a fragment of Amyloid-β peptide.

HY-135336A

(S)-Verapamil hydrochloride (S)-(-)-Verapamil hydrochloride	Leukotriene Receptor Calcium Channel Apoptosis	Cancer
(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.

HY-107743

Naloxone benzoylhydrazone NalBzoH	Opioid Receptor	Neurological Disease
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.

HY-N1968

Quercetin-3-O-β-D-glucose-7-O-β-D-gentiobiosiden Quercetin-3-O-beta-D-glucose-7-O-beta-D-gentiobioside	Others	Others
Quercetin-3-O-β-D-glucose-7-O-β-D-gentiobiosiden is a flavonoid from Quercetin.

HY-125849

Chrysin 7-O-beta-gentiobioside
Chrysin 7-O-β-gentiobioside
Others Cancer

Chrysin 7-O-beta-gentiobioside (Chrysin 7-O-β-gentiobioside) is the glycosylation product of Chrysin.

HY-N6652

*1-beta-D-Arabinofuranosyluracil* Uracil 1-β-D-arabinofuranoside	Others	Cancer Inflammation/Immunology Cardiovascular Disease
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells.

HY-111638

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine
Nucleoside Antimetabolite/Analog Infection

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is a bicyclic nucleoside.

HY-N2056

*11-Keto-beta-boswellic acid* 11-Keto-β-boswellic acid	Lipoxygenase Leukotriene Receptor NF-κB	Cancer
11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.

HY-135864

KRAS inhibitor-6
Ras Cancer

KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
HY-135866

KRAS inhibitor-8
Ras Cancer

KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
HY-135865

KRAS inhibitor-7
Ras Cancer

KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
HY-100260

beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
HIV Infection

beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.

HY-P1504

β-Melanocyte Stimulating Hormone (MSH), human beta-MSH (1-22) (human)	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

HY-114464

*11-Beta-hydroxyandrostenedione* 4-Androsten-11β-ol-3,17-dione	Endogenous Metabolite	Endocrinology
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.

HY-N7035

*Wogonin 7-O-beta-D-glucuronide methyl ester* Wogonoside methyl ester	Others	Metabolic Disease
Wogonin 7-O-beta-D-glucuronide methyl ester is a natural compound isolated from Huanglian Jiedutang.

HY-141139

*1-(Isopropylthio)-2,3,4,6-tetra-o-Ac-beta-D-glucosylpyranose*	PROTAC Linker	Cancer
1-(Isopropylthio)-2,3,4,6-tetra-o-Ac-beta-D-glucosylpyranose is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-12780S

*6-beta-Naloxol D5 hydrochloride* 6β-Naloxol D5 hydrochloride	Opioid Receptor	Neurological Disease
6-beta-Naloxol D5 hydrochloride is the deuterium labeled 6-beta-Naloxol, which is an opioid antagonist closely related to naloxone.

HY-101790

ZM223
NEDD8-activating Enzyme Cancer

ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.

HY-101682B

(R)-SCH 42495	Others	Others
(R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.

HY-A0285

Norethisterone enanthate
Norigest
Progesterone Receptor Endocrinology

Norethisterone enanthate is a long-acting parenteral progestogen. Norethisterone enanthate is orally active.
HY-111902

MCB-3681
Bacterial Infection

MCB-3681 is the antibacterial Oxaquin's active substance, active against gram-positive bacterium.

HY-N0006A

(E/Z)-Demethoxycurcumin p-Hydroxycinnamoyl-feruloylmethane	Others	Inflammation/Immunology Cancer
(E/Z)-Demethoxycurcumin (p-Hydroxycinnamoyl-feruloylmethane) is a curcuminoid isolated from curcuma species, with anticoagulative active.

HY-N0171A

Beta-Sitosterol (purity>98%) β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)	Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-P1504A

β-Melanocyte Stimulating Hormone (MSH), human TFA beta-MSH (1-22) (human) TFA	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

HY-N0171B

Beta-Sitosterol (purity>75%) β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)	Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-N0171

Beta-Sitosterol (purity>80%) β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)	Endogenous Metabolite Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-A0020S

Eldecalcitol-d6	VD/VDR	Metabolic Disease
Eldecalcitol-d6 is the deuterium labeled Eldecalcitol. Eldecalcitol is an orally active analogue of active vitamin D used in the treatment of osteoporosis.

HY-N6675

Gardenia yellow Crocin I	Sirtuin	Neurological Disease Cancer
Gardenia yellow is an active member of crocin, increases mRNA expression of *SIRT3, and acts as an orally active* antidepressant agent.

HY-B0559

Nabumetone BRL14777	COX	Inflammation/Immunology Cancer
Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective *COX-2* inhibitor, and is the prodrug of the active metabolite 6MNA.

HY-101682

SCH 42495	Neprilysin	Cardiovascular Disease
SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.

HY-17620

Sacubitrilat
LBQ-657
Neprilysin Neurological Disease

Sacubitrilat is an active neprilysin (NEP) inhibitor.
HY-U00305

Cicloxilic acid
Cycloxilic acid
Others Inflammation/Immunology

Cicloxilic acid is a biologically active agent.

HY-75041

Calcitriol Impurities A	VD/VDR	Metabolic Disease
Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

HY-77274

Calcitriol Impurities D	VD/VDR	Metabolic Disease
Calcitriol Impurities D is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

HY-100375

Diroximel fumarate ALKS 8700; BIIB098	Others	Others
Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).

HY-A0021C

(R,R)-Palonosetron Hydrochloride
5-HT Receptor Inflammation/Immunology

(R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.

HY-B1069

Molsidomine SIN-10; Morsydomine	Others	Cardiovascular Disease
Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.

HY-N7225

Yuanhuacine Gnidilatidin	Others	Cancer
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.

HY-122872

MKK7-COV-9	p38 MAPK	Cancer
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC₅₀ of 4.98 μM.

HY-15745

PSI-7409	HCV	Cancer
PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.

HY-101682A

SCH 42495 racemate	Neprilysin	Cardiovascular Disease
SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.

HY-13635A

Finasteride acetate
MK-906 acetate
5 alpha Reductase Cancer

Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor.
HY-113161

L-Octanoylcarnitine
Endogenous Metabolite Metabolic Disease

L-Octanoylcarnitine is the physiologically active form of octanoylcarnitine.

HY-13728A

(R)-Plevitrexed (R)-ZD 9331; (R)-BGC9331	Others	Cancer
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.

HY-100373

Isavuconazonium sulfate BAL8557-002	Fungal	Infection
Isavuconazonium sulfate (BAL8557-002), the prodrug of the active triazole Isavuconazole, is an orally active antifungal agent. Isavuconazonium sulfate is used for invasive aspergillosis and mucormycosis.

HY-18627A

PFI-2 hydrochloride (R)-PFI-2 hydrochloride	Histone Methyltransferase	Cancer
PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.

HY-133771AS

Nordoxepin D3 hydrochloride Desmethyldoxepin D3 hydrochloride	Drug Metabolite	Neurological Disease
Nordoxepin D3 hydrochloride (Desmethyldoxepin D3 hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant.

HY-18627

PFI-2 (R)-PFI-2	Histone Methyltransferase	Cancer
PFI-2 is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.

HY-N0724

Mesaconitine
TNF Receptor Others

Mesaconitine is the main active component of genus aconitum plants.
HY-16500

Tolrestat
AY-27773
Aldose Reductase Cancer

Tolrestat is a potent, orally active aldose reductase inhibitor with IC₅₀ of 35 nM.
HY-N2097

Cimigenoside
Others Metabolic Disease

Cimigenoside is an active compound from genus Cimicifuga.
HY-14864A

(S)-Mapracorat
(S)-ZK-245186; (S)-BOL-303242X
Glucocorticoid Receptor Endocrinology

(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.

HY-N0560

Oroxylin A Baicalein 6-methyl ether; 6-Methoxybaicalein	HIF/HIF Prolyl-Hydroxylase Autophagy Virus Protease	Cancer
Oroxylin A is a natural active flavonoid with strong anticancer effects.

HY-U00358

Compound 2
Others Metabolic Disease

Compound 2 is an active compound used for the research of metabolic bone diseases.
HY-75958

Vitamin D4
VD/VDR Metabolic Disease

Vitamin D4 is the active analogue of Vitamin D.
HY-U00041

Pivalopril
Pivopril; RHC 3659(S)
Angiotensin-converting Enzyme (ACE) Cardiovascular Disease

Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.
HY-13635

Finasteride
MK-906
5 alpha Reductase Cancer

Finasteride is an orally active testosterone 5-alpha-reductase inhibitor (Ki= 10 nM).
HY-100406

(S)-MCPG
(+)-MCPG
mGluR Neurological Disease

(S)-MCPG is the active isomer of (RS)-MCPG (Cat.

HY-13293

Impurity C of Calcitriol	VD/VDR	Cancer
Impurity C of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

HY-13292

Impurity B of Calcitriol 1β,25-Dihydroxyvitamin-D3; 1-Epicalcitriol	VD/VDR	Cancer
Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

HY-111386

E-7386
Epigenetic Reader Domain Cancer

E-7386 is an orally active CBP/beta-catenin modulator.
HY-13735D

d-Atabrine dihydrochloride
Bacterial Infection

d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.

HY-G0002A

Lurasidone metabolite 14326 hydrochloride	Drug Metabolite	Neurological Disease
Lurasidone metabolite 14326 (hydrochloride) is an active metabolite of the atypical antipsychotic Lurasidone.

HY-101203A

GJ103 sodium salt
Others Others

GJ103 sodium salt is an active analog of the read-through compound GJ072.
HY-U00389

WQ3810
KPI-10 free base
Bacterial Infection

WQ3810 is an orally active fluoroquinolone, with potent antibacterial activities.
HY-N0076

Bilobalide
(-)-Bilobalide
Autophagy Endogenous Metabolite Neurological Disease

Bilobalide is a biologically active terpenic trilactone present in Ginkgo biloba.
HY-112104

Meta-Topolin
m-Topolin
Others Others

Meta-Topolin (m-Topolin) is a highly active aromatic cytokinin.
HY-14645B

DHMEQ racemate
rel-DHMEQ
NF-κB Cancer

DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ.
HY-B1103

Hydroxyhexamide
(±)-Hydroxyhexamid
Drug Metabolite Cardiovascular Disease

Hydroxyhexamide is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agents.

HY-18719B

Endoxifen hydrochloride	Estrogen Receptor/ERR Drug Metabolite Parasite	Cancer
Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor.

HY-B0257

Levonorgestrel
D-Norgestrel
Progesterone Receptor Endocrinology

Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives.
HY-N0238

Atractylodin
Atractydin
Others Others

Atractylodin is an active component of the essential oil contained in the rhizomes of Atractylodes lancea and A.
HY-G0002

Lurasidone metabolite 14326
Drug Metabolite Neurological Disease

Lurasidone metabolite 14326 is an active metabolite of the atypical antipsychotic Lurasidone.
HY-14885

Eliglustat
Genz 99067
Others Metabolic Disease

Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC₅₀ of 24 nM.

HY-133781

cis-Clopidogrel-MP Derivative Clopidogrel-MP-AM	Others	Others
cis-Clopidogrel-MP Derivative (Clopidogrel-MP-AM) is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor.

HY-B1210

Pipemidic acid
Bacterial Antibiotic Infection

Pipemidic scid is a new antibacterial agent, is active against Pseudomonas aeruginosa.
HY-N0519

Calycosin
Cyclosin
Apoptosis Cancer

Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.
HY-17044A

Duvelisib R enantiomer
IPI-145 R enantiomer; INK1197 R enantiomer
PI3K Cancer

Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.

HY-13667

Levoleucovorin Calcium Calcium levofolinate; CL307782	Antifolate	Cancer
Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.

HY-111068

KD-3010
PPAR Metabolic Disease

KD-3010 is a potent, orally active, and selective PPARδ agonist.
HY-75957

DMP 777
L-694458
Elastase Inflammation/Immunology

DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
HY-B0490

Hygromycin B
Hygrovetine
Bacterial Fungal Antibiotic Infection

Hygromycin B is an aminoglycoside antibiotic active against prokaryotic and eukaryotic cells.
HY-108694

γ-Tocotrienol
Others Metabolic Disease Inflammation/Immunology

γ-Tocotrienol is an active form of vitamin E.
HY-U00075

Indanazoline
Others Cardiovascular Disease

Indanazoline (as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action.
HY-101739

Amcinafal
SQ 15102
Others Infection

Amcinafal is an active diol, used against virus replication and interferon production.
HY-14916

Camobucol
AGIX 4207
Others Inflammation/Immunology

Camobucol is an orally active, phenolic antioxidant and anti-inflammatory compound with antirheumatic properties.
HY-19163

SC-52012
Others Cardiovascular Disease

HY-19163 is an orally active fibrinogen receptor antagonist, with antiplatelet activities.

HY-N0752

Scutellarein 6-Hydroxyapigenin; 4',5,6,7-Tetrahydroxyflavone	Src Autophagy SARS-CoV	Inflammation/Immunology Cancer
Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.

HY-106067A

Dazoxiben
Prostaglandin Receptor Inflammation/Immunology

Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor.

HY-14885A

Eliglustat hemitartrate Genz-112638; Eliglustat tartrate	Others	Metabolic Disease
Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC₅₀ of 24 nM.

HY-14798

Palifosfamide Isophosphoramide mustard; IPM; ZIO-201	DNA Alkylator/Crosslinker Drug Metabolite	Cancer
Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.

HY-19323

Ceralasertib
AZD6738
ATM/ATR Cancer

Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC₅₀ of 1 nM.
HY-13735C

l-Atabrine dihydrochloride
Bacterial Infection

l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.

HY-76814

Calcitriol D6	VD/VDR	Metabolic Disease
Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

HY-70002A

N-desmethyl Enzalutamide N-desmethyl MDV 3100	Androgen Receptor	Cancer
N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide.

HY-15246

TAK-580
MLN 2480; BIIB-024
Raf Cancer

TAK-580 (MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.
HY-17492

Zafirlukast
ICI 204219
Leukotriene Receptor Inflammation/Immunology Cancer

Zafirlukast is a potent orally active leukotriene D₄ (LTD₄) receptor antagonist.

HY-13079

Cobimetinib R-enantiomer GDC-0973 R-enantiomer; XL-518 R-enantiomer	MEK	Cancer
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

HY-U00332

Hydrocarbon chain derivative 1 6,6'-Oxybis[2,2-dimethyl-1-hexanol]	Others	Metabolic Disease
Hydrocarbon chain derivative 1 is an active compound, with inhibitory activities against lipid synthesis.

HY-B2223

Thiamine nitrate
Vitamin B1 nitrate
Others Metabolic Disease

Thiamine nitrate is an essential vitamin which can enhance normal neuronal actives.
HY-16445B

CNDAC hydrochloride
Nucleoside Antimetabolite/Analog Drug Metabolite Cancer

CNDAC hydrochloride is a metabolite of the orally active agent sapacitabine, and a nucleoside analog.
HY-18958

CCT245737
Checkpoint Kinase (Chk) Cancer

CCT245737 is an orally active and seletive Chk1 inhibitor, with an IC₅₀ of 1.3 nM.

HY-B0331A

Enalapril maleate MK-421 maleate	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Enalapril (maleate) (MK-421 (maleate)), the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.

HY-B0332

Menadione
Vitamin K3
Endogenous Metabolite Others

Menadione, a synthetic naphthoquinone, can be converted to active vitamin K2 in vivo.
HY-A0246A

Flucloxacillin sodium
Bacterial Antibiotic Infection

Flucloxacillin sodium is a highly active antibiotic against Gram-positive and Gram-negative bacteria.
HY-79593

MRE-269
ACT-333679
Prostaglandin Receptor Cardiovascular Disease Endocrinology

MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
HY-101830

Wy 49051
Histamine Receptor Inflammation/Immunology Endocrinology

Wy 49051 is a potent, orally active H1 receptor antagonist, with IC₅₀ of 44 nM.

HY-77591

Cysteamine hydrochloride β-Mercaptoethylamine Hydrochloride; 2-Aminoethanethiol Hydrochloride; 2-Mercaptoethylamine Hydrochloride; Thioethanolamine Hydrochloride	Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite	Metabolic Disease Cancer
Cysteamine hydrochloride (β-Mercaptoethylamine Hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.

HY-N0053

Psoralen
Furocoumarin; Ficusin
Apoptosis HIV Influenza Virus Cancer

Psoralen (Furocoumarin) is an active ingredient from Fructus Psoraleae; has anticancer activity.
HY-112066A

(+)-SHIN1
(+)-RZ-2994
Others Others

(+)-SHIN1 ((+)-RZ-2994) is an active (+) enantiomer of SHIN1.
HY-B1229

Isovaleramide
3-Methylbutanamide
Others Neurological Disease

Isovaleramide is an active principle on central nervous system from Valeriana pavonii, as an anticonvulsant.

HY-77591A

Cysteamine β-Mercaptoethylamine; 2-Aminoethanethiol; 2-Mercaptoethylamine	Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite	Cancer Metabolic Disease
Cysteamine (β-Mercaptoethylamine) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.

HY-A0020

Eldecalcitol ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3	VD/VDR	Metabolic Disease
Eldecalcitol (ED-71) is an orally active analogue of active vitamin D used in the treatment of osteoporosis. Eldecalcitol (ED-71) possesses a strong inhibitory effect on bone resorption and causes a significant increase in bone mineral density.

HY-B0510

Trimethoprim	Antifolate Bacterial Antibiotic	Infection
Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.

HY-101877

Statine (3S,4S)-Statine; (S,S)-Statine	Others	Endocrinology
Statine is an unusual amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases.

HY-N0565

Doxycycline
MMP Bacterial Parasite Antibiotic Infection

Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-19563

A-893
Histone Methyltransferase Cancer

A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC₅₀ of 2.8 nM.
HY-B0924

Anisindione
Others Cardiovascular Disease

Anisindione is a synthetic anticoagulant, prevents the formation of active procoagulation factors II, VII, IX, and X.
HY-N0565A

Doxycycline hydrochloride
MMP Bacterial Antibiotic Infection

Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-12784

Cycloguanil
Parasite Drug Metabolite Infection

Cycloguanil, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes.
HY-106446

Rentiapril
SA-446
Angiotensin-converting Enzyme (ACE) Cardiovascular Disease

Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
HY-13320

2-Keto Crizotinib
PF-06260182
ALK Cancer

2-Keto Crizotinib (PF-06260182) is an active lactam metabolite of crizotinib.

HY-11103

Sitaxsentan sodium IPI 1040 sodium; TBC11251 sodium	Endothelin Receptor	Cardiovascular Disease Endocrinology
Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.

HY-N0886

Aloin B
Aloin-B; Isobarbaloin
Others Others

Aloin B is one isomer of Aloin; Aloin is a physiologically active anthraquinone present in aloe.
HY-15333

ZK-261991
VEGFR Inflammation/Immunology

ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC₅₀ of 5 nM for VEGFR2.
HY-125850

Berberrubine chloride
Others Inflammation/Immunology

Berberrubine chloride is an active metabolite of berberine, attenuates ulcerative colitis in mice model.
HY-N6988

Cimigenol
Others Cancer

Cimigenol is an active compound isolated from Cimicifuga, with potent anti-tumor activity.

HY-P0198

Neuropeptide Y (29-64), amide, human Human neuropeptide Y (29-64)	Neuropeptide Y Receptor	Neurological Disease Endocrinology
Neuropeptide Y (29-64), amide, human is a biologically active 36-amino acid peptide.

HY-118861A

Enclomiphene citrate (E)-Clomiphene citrate; trans-Clomiphene citrate; Enclomifene citrate	Estrogen Receptor/ERR	Inflammation/Immunology
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.

HY-B0550

Bismuth Subsalicylate Bismuth oxysalicylate; Bismuth(III) salicylate basic	PGE synthase	Neurological Disease
Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.

HY-12784A

Cycloguanil hydrochloride
Parasite Drug Metabolite Infection

Cycloguanil hydrochloride, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes.
HY-10002

Calcitriol
1,25-Dihydroxyvitamin D3
VD/VDR Endogenous Metabolite Cancer

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

HY-P0128

β-Amyloid (25-35) Amyloid beta-peptide (25-35); Aβ25-35; β-Amyloid peptide (25-35)	Amyloid-β	Neurological Disease
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.

HY-B0510C

Trimethoprim lactate	Antifolate Bacterial	Infection
Trimethoprim lactic is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactic is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactic has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.

HY-117244

AZD7507
c-Fms Cancer

AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.
HY-N1479

Polygalic acid
Others Others

Polygalic acid, a triterpenoid saponin, is considered one of the major active constituents of Polygala tenuifolia.
HY-B0810

Pivmecillinam
FL-1039
Bacterial Antibiotic Infection

Pivmecillinam (FL-1039) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.

HY-B0810A

Pivmecillinam hydrochloride FL-1039 hydrochloride	Bacterial Antibiotic	Infection
Pivmecillinam hydrochloride (FL-1039 hydrochloride) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.

HY-100318

NGD-4715
MCHR1 (GPR24) Metabolic Disease Endocrinology

NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
HY-135400

Glyco-Obeticholic acid
FXR Inflammation/Immunology

Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
HY-101982

Lys-SMCC-DM1
Lys-Nε-MCC-DM1
Drug-Linker Conjugates for ADC Cancer

Lys-SMCC-DM1 is the active metabolite of DM1. DM1 is a tubulin inhibitor.

HY-N1944

Nerolidol	Bacterial Fungal Parasite Endogenous Metabolite	Cancer Infection
Nerolidol is a natural membrane-active sesquiterpene, with antitumor, antibacterial, antifungal and antiparasitic activity.

HY-13038A

Fostamatinib
R788
Syk Inflammation/Immunology Cancer

Fostamatinib (R788), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

HY-B1056

Procodazole Propazol; 2-Benzimidazolepropionic acid	Bacterial	Infection
Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections, used as a potentiator.

HY-B0016

Capecitabine	DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis	Cancer
Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.

HY-B1323

Dipivefrin hydrochloride Dipivefrine hydrochloride	Others	Neurological Disease
Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma prodrug that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea.

HY-B1391

D-Panthenol Dexpanthenol	Endogenous Metabolite	Inflammation/Immunology Cancer
D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.

HY-12023

Andarine
GTx-007; S-4
Androgen Receptor Cancer

Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.

HY-B0277

Vidarabine Ara-A; Adenine Arabinoside; 9-β-D-Arabinofuranosyladenine	HSV Nucleoside Antimetabolite/Analog Antibiotic	Infection
Vidarabine (Ara-A) an antiviral drug which is active against herpes simplex and varicella zoster viruses.

HY-135279

CFTR corrector 4	CFTR	Inflammation/Immunology
CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.

HY-19851

Rovafovir etalafenamide GS-9131	Reverse Transcriptase HIV	Cancer
Rovafovir etalafenamide (GS-9131), a prodrug of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity.

HY-W013186S

Lansoprazole Sulfide D4	Proton Pump Bacterial	Inflammation/Immunology
Lansoprazole Sulfide D4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (*Mycobacterium tuberculosis) agent with IC₅₀* values of 0.59 µM intracellularly and 0.46 µM in broth.

HY-10109

AS-605240
PI3K Autophagy Cancer

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC₅₀ of 8 nM, and a K_i of 7.8 nM.
HY-70037

Cinacalcet
AMG 073
CaSR Cardiovascular Disease

Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-B0257A

Dydrogesterone	Progesterone Receptor	Endocrinology
Dydrogesterone is a potent, orally active progestogen indicated in a wide variety of gynaecological conditions related to progesterone deficiency.

HY-76082

L-Pyroglutamic acid	Endogenous Metabolite	Others
L-Pyroglutamic acid is the levo-isomer of Pyroglutamic acid. L-Pyroglutamic acid is the biologically active enantiomer in humans. Pyroglutamic acid is an intermediate in glutathione metabolism.

HY-N0860

Schisantherin E Schizantherin-E	Others	Inflammation/Immunology
Schisantherin E is a natural compound isolated from the active fraction of the fruits of Schisandra sphenanthera Rehd. et Wils.

HY-I0447

4-Aminosalicylic acid
Bacterial Antibiotic Infection Inflammation/Immunology

4-Aminosalicylic acid (ASA) is an orally active antibiotic and has the potential to treat tuberculosis.
HY-13059B

SDZ 220-581 hydrochloride
iGluR Neurological Disease

SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pK_i value of 7.7.

HY-12872B

Nazartinib S-enantiomer EGF816 (S-enantiomer)	Others	Others
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.

HY-N0267

Hypaconitine
TNF Receptor Inflammation/Immunology

Hypaconitine, an active and highly toxic constituent derived from Aconitum species, is widely used to treat rheumatism.

HY-G0001A

Lurasidone Metabolite 14283 hydrochloride	Drug Metabolite	Neurological Disease
Lurasidone Metabolite 14283 hydrochloride is a major active metabolite of Lurasidone. Lurasidone is a FDA approved drug for the treatment of schizophrenia.

HY-N4290

3-Epioleanolic acid
Others Inflammation/Immunology

3-Epioleanolic acid is an active component of Verbena officinalis Linn, with anti-inflammatory activity.
HY-19487A

Ribocil B
Ribocil S enantiomer; ent-Ribocil A
Bacterial Infection

Ribocil-B is the active S-isomer of ribocil which can inhibit flavin mononucleotide (FMN) with a K_D of 6.6 nM.
HY-13059

SDZ 220-581
iGluR Neurological Disease

SDZ 220-581 is an orally active, potent, competitive NMDA receptor antagonist with pK_i value of 7.7.
HY-100600

BGG463
K03859
CDK Others

BGG463 (K03859) is an orally active type II CDK2 inhibitor.
HY-18966

PF-04418948
Prostaglandin Receptor Cancer Endocrinology

PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC₅₀ of 16 nM.
HY-12075

LY2109761
TGF-β Receptor Autophagy Cancer

LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with K_is of 38 nM and 300 nM, respectively.
HY-12886

Docebenone
AA 861
Lipoxygenase Ferroptosis Inflammation/Immunology

Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.

HY-A0058

Retinyl glucoside Retinyl β-D-glucoside	Others	Metabolic Disease
Retinyl-β-D-glucoside is a naturally occurring and biologically active metabolites of vitamin A, which are found in fish and mammals.

HY-B1744

Pyridoxal phosphate Pyridoxal 5′-phosphate; Pyridoxyl phosphate	Reverse Transcriptase Endogenous Metabolite	Neurological Disease
Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia.

HY-114157

DO-264
MAGL Neurological Disease

DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC₅₀ of 11 nM.
HY-W011651

Carbutamide
BZ-55
Others Metabolic Disease

Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity.
HY-18607

SGK1-IN-1
SGK Inflammation/Immunology

SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC₅₀ of 1 nM.
HY-100269

Chymase-IN-1
Others Inflammation/Immunology

Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC₅₀ of 29 nM.
HY-U00084

SUN 1334H
Histamine Receptor Inflammation/Immunology Endocrinology

SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with K_i of 9.7 nM.
HY-19274

ZD-1611
Endothelin Receptor Cardiovascular Disease Endocrinology

ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.

HY-135394

3-Desacetyl Cefotaxime lactone	Drug Metabolite	Infection
3-Desacetyl Cefotaxime lactone is the active metabolite of Cefotaxime. Cefotaxime sodium salt is a third-generation cephalosporin antibiotic.

HY-20685

Impulsin AM 3112; Loramine P 256; Mackpeart DR 14V	Influenza Virus Endogenous Metabolite	Infection
Impulsin (AM 3112) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.

HY-126295

Anti-parasitic agent 3
Parasite Infection

Anti-parasitic agent 3 is an anti-parasitic agent which active against drug resistant parasites.
HY-114397

SHP394
Phosphatase Cancer

SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC₅₀ of 23 nM.
HY-U00039

Desethyl KBT-3022
Thrombin Cardiovascular Disease

Desethyl KBT-3022 is the main active metabolite of the new antiplatelet agent, KBT-3022.
HY-14751

Rolapitant
SCH619734
Neurokinin Receptor Cancer Endocrinology

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a K_i of 0.66 nM.

HY-18719E

Endoxifen	Estrogen Receptor/ERR Aromatase	Cancer
Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity.

HY-B1761

Santonin
Alpha-Santonin
Parasite Infection

Santonin is an active principle of the plant Artemisia cina, which is formely used to treat worms.

HY-B0568

Deferiprone	HCV Ferroptosis	Cardiovascular Disease Cancer
Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload.

HY-100435

Oxaquin MCB-3837; DNV3837	Bacterial	Infection
Oxaquin (MCB-3837) is a water-soluble, injectable prodrug that is rapidly converted to the active sub-stance MCB3681 in vivo following intravenous (i.v.) administration, active against Gram-positive bacterial species. Oxaquin (MCB-3837) itself has no antimicrobial effects.

HY-10791

Ritanserin R 55667	5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT₂ receptor, with an IC₅₀ of 0.9 nM, less active on Histamine H₁, Dopamine D₂, Adrenergic α₁, Adrenergic α₂ receptors.

HY-N6006

*1,3,6-Tri-O-galloyl-beta-D-glucose* 1,3,6-Tri-O-galloyl-β-D-glucose	Others	Others
1,3,6-Tri-O-galloyl-beta-D-glucose (1,3,6-Tri-O-galloyl-β-D-glucose) is a phenolic compound in Black Walnut Kernels.

HY-N0818

Chikusetsusaponin Iva Calenduloside F	Others	Others
Chikusetsusaponin IVa a major active ingredient of triterpenoid saponins, exerts antithrombotic effects, including minor hemorrhagic events.

HY-112853

Fosmidomycin sodium salt FR-31564	Bacterial Antibiotic	Infection
Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial drug, which is active against both Gram-negative and Gram-positive bacteria.

HY-100742B

(S)-GNE-140
Lactate Dehydrogenase Cancer

(S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).

HY-N0565B

Doxycycline (hyclate) Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031	MMP Bacterial Antibiotic	Infection
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.

HY-16232

GLUFOSFAMIDE D 19575; Glucosylifosfamide mustard	Others	Cancer
Glufosfamide is a novel alkylating agent in which the active metabolite of isophosphoramide mustard is glycosidically linked to β-D-glucose.

HY-B0688

Dapsone 4,4′-Diaminodiphenyl sulfone; DDS	Bacterial Reactive Oxygen Species Antibiotic	Infection
Dapsone is a sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.

HY-N6039

Gentianine
Others Metabolic Disease Inflammation/Immunology

Gentianine, an active metabolite of Swertiamarin, has anti-diabetic effect and anti-inflammatory property.
HY-103407A

PD 168568 dihydrochloride
Dopamine Receptor Neurological Disease

PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a K_i of 8.8 nM.
HY-102053

Apimostinel
NRX-1074; AGN-241660
iGluR Neurological Disease

Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.
HY-18698

L-701324
iGluR Neurological Disease

L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.
HY-131142

Monensin methyl ester
Others Others

Monensin methyl ester, a neutral analog of monensin, is an ion active component for Na+ selective disk electrodes.
HY-32350

Ercalcitriol
1α,25-Dihydroxy Vitamin D2
VD/VDR Drug Metabolite Endogenous Metabolite Metabolic Disease

Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.

HY-B1080

Tilorone dihydrochloride	HIF/HIF Prolyl-Hydroxylase Influenza Virus	Infection Cancer
Tilorone dihydrochloride is the first recognized synthetic, small molecular weight compound that is an orally active interferon inducer, used as an antiviral drug.

HY-106571

Cefteram pivoxil
Ro 19-5248; T-2588
Bacterial Infection

Cefteram pivoxil (Ro 19-5248), an orally active cephalosporin antibiotic, is used for bacterial infections.

HY-135399

Tauro-Obeticholic acid	FXR	Inflammation/Immunology
Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.

HY-14336A

SB 271046 Hydrochloride
SB 271046A
5-HT Receptor Neurological Disease

SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
HY-13059A

SDZ 220-581 Ammonium salt
iGluR Neurological Disease

SDZ 220-581 Ammonium salt is an orally active, potent, competitive NMDA receptor antagonist with pK_i value of 7.7.
HY-100754

PF-06651600
JAK Inflammation/Immunology

PF-06651600 is an orally active and selective JAK3 inhibitor with an IC₅₀ of 33.1 nM.
HY-U00148

KY-556
N556
Others Inflammation/Immunology

KY-556 is a promising and orally-active pro-drug of disodium cromoglycate (DSCG) against allergic diseases.
HY-N6728

Helvolic acid
Fumigacin
Bacterial Infection

Helvolic acid (Fumigacin) is an antibiotic isolated from Xylaria sp, active against the Gram-positive bacteria.
HY-114307

Ly93
Others Inflammation/Immunology

Ly93 is a selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with an IC₅₀ of 91 nM.

HY-100584

Davercin Erythromycin Cyclocarbonate	Bacterial Antibiotic	Infection
Davercin (Erythromycin Cyclocarbonate), derivative of Erythromycin, which is active against Gram-positive and some Gram-negative microorganisms.

HY-70037A

Cinacalcet hydrochloride AMG-073 hydrochloride	CaSR	Cardiovascular Disease
Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-A0070

Liothyronine sodium Triiodothyronine sodium; 3,3',5-Triiodo-L-thyronine sodium; T3 sodium	Thyroid Hormone Receptor	Cancer Endocrinology
Liothyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

HY-B1417

Nortriptyline hydrochloride Desmethylamitriptyline hydrochloride	Autophagy Apoptosis Drug Metabolite	Neurological Disease Cancer
Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression.

HY-B0794A

AZ7550 hydrochloride
IGF-1R Drug Metabolite Cancer Endocrinology

AZ7550 hydrochloride is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.
HY-112166

PRN1008
Btk Cancer Metabolic Disease

PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC₅₀ of 1.3 nM.
HY-110255

AZD 2066
mGluR Neurological Disease

AZD 2066 is a selective, orally active and brain-penetrant mGluR5 antagonist, with analgesia activity.
HY-10285

Saxagliptin
BMS-477118
Dipeptidyl Peptidase Metabolic Disease

Saxagliptin is an orally active dipeptidyl peptidase-4 (DPP4) inhibitor that helps control blood sugar levels.
HY-N1399

Androsin
Others Inflammation/Immunology

Androsin is an active compound isolated from Picrorhiza Kurroa Royle ex Benth, with anti-asthmatic effects.

HY-13038

Fostamatinib Disodium R788(Disodium)	Syk	Inflammation/Immunology Cancer
Fostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

HY-100856

PCO371
Thyroid Hormone Receptor Endocrinology

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.

HY-A0070A

Liothyronine Triiodothyronine; 3,3',5-Triiodo-L-thyronine; T3	Thyroid Hormone Receptor Endogenous Metabolite	Cancer Endocrinology
Liothyronine is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

HY-B0794

AZ7550
IGF-1R Drug Metabolite Cancer Endocrinology

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.
HY-100423A

Eltanexor Z-isomer
KPT-8602 (Z-isomer)
CRM1 Cancer

Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
HY-U00008

CP-28888
CP 28888-27
Others Infection

CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
HY-101803

CP671305
Phosphodiesterase (PDE) Others

CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.

HY-19191

L-159282 MK 996	Angiotensin Receptor	Cardiovascular Disease Endocrinology
L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.

HY-101583

NEO 376 SPI-376	5-HT Receptor GABA Receptor Dopamine Receptor	Neurological Disease
NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.

HY-12687

Tizoxanide TIZ	Bacterial HIV Autophagy	Infection
Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses.

HY-B0794B

AZ7550 Mesylate AZ7550 trimesylate salt	IGF-1R Drug Metabolite	Cancer Endocrinology
AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

HY-76938

Actarit 4-Acetylaminophenylacetic acid; MS-932	Others	Inflammation/Immunology
Actarit, an orally active antirheumatic compound, has the potential to treat type II collagen-induced arthritis.

HY-17629

Dapansutrile	NOD-like Receptor (NLR)	Inflammation/Immunology
Dapansutrile is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity.

HY-100988

Methylergometrine maleate Methylergonovine maleate; Ryegonovin; Spametrin F	5-HT Receptor	Neurological Disease
Methylergometrine maleate (Methylergonovine maleate) is an ergot alkaloid and an active metabolite of Methysergide with vasoconstrictive and uterotonic activity. Methylergometrine maleate is a potent, selective and orally active 5-HT receptors antagonist with a *pA₂* value of 9.6. Methylergometrine maleate has antimigraine and dopaminergic activity. Methylergometrine maleate can used for the prevention and control of postpartum hemorrhage.

HY-108425A

AMG8380	Sodium Channel	Neurological Disease
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC₅₀s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC₅₀ of 2560 nM.

HY-109008

Nacubactam OP0595 free acid	Bacterial	Infection
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs.

HY-15233

Letermovir
AIC246
CMV Infection

Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
HY-112945

MLS0315771
Others Metabolic Disease

MLS0315771 is a potent and biologically active competitive phosphomannose isomerase (MPI) inhibitor, with an IC₅₀ ~1 μM and a K_i of 1.4 μM.
HY-U00359

LTD4 antagonist 1
Leukotriene Receptor Inflammation/Immunology

LTD₄ antagonist 1 is a potent, orally active antagonist of leukotriene D₄ (LTD₄) with a K_i of 0.57 nM.

HY-B1583

(Z)-Capsaicin Zucapsaicin; Civamide; cis-Capsaicin	TRP Channel HSV	Neurological Disease
(Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.

HY-111418

EBI-2511
Histone Methyltransferase Cancer

EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC₅₀ of 6 nM in Pfeffiera cell lines, respectively.
HY-131060

CN128
Others Others

CN128 is an orally active and selective iron chelator. CN128 is used for the research of β-thalassemia.

HY-B0022

Flutamide SCH 13521	Androgen Receptor	Cancer
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

HY-50736

DUB-IN-1
Deubiquitinase Cancer

DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC₅₀ of 0.24 μM for USP8.
HY-128576

DS21360717
Others Cancer

DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC₅₀ of 0.49 nM. Anti-cancer activity.
HY-16715

Acumapimod
p38 MAPK Autophagy Inflammation/Immunology

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC₅₀ of less than 1 μM for p38α.

HY-114258

LY3295668 AK-01	Aurora Kinase	Cancer
LY3295668 is a potent, orally active and highly specific Aurora-A kinase inhibitor, with K_i values of 0.8 nM and 1038 nM for AurA and AurB, respectively.

HY-B0798

Cefpiramide sodium SM-1652; Wy-44635	Bacterial Antibiotic	Infection
Cefpiramide sodium (SM-1652; Wy-44635) is a new Pseudomonas-active cephalosporin with a broad spectrum of antibacterial activity.

HY-A0009

Galanthamine hydrobromide Galantamine hydrobromide	AChE Apoptosis	Neurological Disease
Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.

HY-111748

RORγt Inverse agonist 2
ROR Inflammation/Immunology

RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC₅₀ of 119 nM.
HY-18012

Spebrutinib
AVL-292; CC-292
Btk Cancer

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC₅₀ of 0.5 nM.

HY-12279F

Umbralisib R-enantiomer TGR-1202 R-enantiomer; RP5264 R-enantiomer	PI3K	Cancer
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a *PI3Kδ* inhibitor, which is the less active enantiomer of TGR-1202.

HY-16950B

(E)-4-Hydroxytamoxifen
Estrogen Receptor/ERR Cancer

(E)-4-Hydroxytamoxifen, the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
HY-Y0078

Cinnamyl Alcohol
PPAR Metabolic Disease

Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity.
HY-125965

BioA-IN-13
Bacterial Infection

BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.

HY-N0424

Cycloastragenol Cyclogalagenin; Cyclogalegenin; Cyclogalegigenin	Others	Others
Cycloastragenol, a natural tetracyclic triterpenoid, was first identified when screening Astragalus membranaceus extracts for active ingredients with antiaging properties.

HY-N0195

Azomycin
2-Nitroimidazole
Bacterial Antibiotic Infection

Azomycin (2-Nitroimidazole) is an antibiotic which can be active against aerobic Gram-positive and Gram-negative bacteria.
HY-18767A

(R,S)-Ivosidenib
(R,S)-AG-120
Isocitrate Dehydrogenase (IDH) Cancer

(R,S)-Ivosidenib ((R,S)-AG-120) is the less active enantiomer of Ivosidenib (AG-120).

HY-15601

Vesatolimod GS-9620	Toll-like Receptor (TLR) Apoptosis HBV HCV HIV	Inflammation/Immunology
Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC₅₀ of 291 nM.

HY-15778

AVE 0991
Angiotensin Receptor Cardiovascular Disease Endocrinology

AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC₅₀ of 21 nM.
HY-19727A

FOY 251
Others Metabolic Disease

FOY 251 is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.
HY-126085

(±)-Alliin
(±)-L-Alliin
SARS-CoV Infection

(±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (M_pro).
HY-100894

Biotin-VAD-FMK
Caspase Cancer

Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.

HY-N1913

Danshensu Dan shen suan A; Salvianic acid A	Keap1-Nrf2 Autophagy Apoptosis	Cardiovascular Disease Cancer
Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating *Nrf2* signaling pathway.

HY-16346

Netupitant CID 6451149	Neurokinin Receptor	Neurological Disease Endocrinology
Netupitant (CID-6451149) is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.

HY-121235

Clonixin
SCH-10304
Others Inflammation/Immunology

Clonixin (SCH-10304) is an orally active analgesic and a non-steroidal anti-inflammatory agent in rodents.
HY-101812

Terbufibrol
Others Metabolic Disease

Terbufibrol has been shown highly active in reducing serum total cholesterol (TC) levels in the normal and hypercholesterolemic male rat.
HY-19097

Ro-24-4736
Others Cardiovascular Disease

Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
HY-U00022

RWJ 63556
COX Lipoxygenase Inflammation/Immunology

RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.
HY-101726

DuP 105
Bacterial Infection

DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.

HY-16901A

Firsocostat S enantiomer ND-630 S enantiomer; GS-0976 S enantiomer; NDI-010976 S enantiomer	Others	Others
Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase (ACC) inhibitor.

HY-15243

Capromorelin Tartrate CP 424391-18	GHSR	Neurological Disease Endocrinology
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

HY-15961

Antitumor agent-3
Others Cancer

Antitumor agent-3 is a potent compound which comprises a new imidazopyridine having excellent antitumor activity as an active ingredient.
HY-N6971

Cimiracemoside C
Cimicifugoside M
AMPK Metabolic Disease

Cimiracemoside C is an active component of Cimicifuga racemosa, activates AMPK, has the potential activity against diabetes.

HY-N0246

Saikosaponin A	LXR Bacterial	Inflammation/Immunology Cancer
Saikosaponin A is an active component of Bupleurum falcatum, up-regulates LXRα expression, with potent anti-inflammatory activity.

HY-108869

Fodipir DPDP	Others	Inflammation/Immunology
Fodipir is an active metabolite of mangafodipir, involved in mangafodipir-mediated cytoprotection against 7β-hydroxycholesterol-induced cell death.

HY-100239

ICI 153110	Phosphodiesterase (PDE)	Cardiovascular Disease
ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.

HY-107831

5-Acetylsalicylic acid
Others Inflammation/Immunology

5-Acetylsalicylic acid has anti-inflammatory and is considered to be the active agent in inflammatory bowel disease (IBD).

HY-136588

trans-R-138727MP Prasugrel metabolite R-138727MP	P2Y Receptor	Cardiovascular Disease
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.

HY-136109A

SEP-363856 SEP-856	5-HT Receptor	Neurological Disease
SEP-363856 （SEP-856）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 （SEP-856） has the potential for the treatment of schizophrenia.

HY-A0019

Paliperidone 9-Hydroxyrisperidone	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

HY-B1973

Diflubenzuron	Others	Others
Diflubenzuron, the active ingredient of the insecticide Dimilin, is a chitin-synthesis inhibiting insecticide. Diflubenzuron possesses larvicidal and ovicidal activities.

HY-B1275

Cephalothin sodium Cefalotin sodium	Bacterial Antibiotic	Infection
Cephalothin sodium is a first generation cephem antibiotic with a wide range antibacterial activity, is active against gram-positive and gram-negative bacteria.

HY-16735

Avoralstat
BCX4161
Others Others

Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.

HY-N3962

Glycyrrhisoflavone	Glucosidase	Metabolic Disease
Glycyrrhisoflavone, an active prenylflavonoid, mainly derived from the extract of the roots of Glycyrrhiza uralensis Fisch.. Glycyrrhisoflavone inhibits α-glucosidase.

HY-108251

Methotrexate metabolite DAMPA	Antifolate Drug Metabolite	Inflammation/Immunology
Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.

HY-N7111

Sultamicillin tosylate	Bacterial	Infection
Sultamicillin (tosylate) is a potent and orally active beta-lactamase inhibitor, an antibiotic with antibacterial activity. Sultamicillin (tosylate) is the tosylate salt of the double ester of sulbactam plus ampicillin.

HY-N0739

Betaine hydrochloride betaine chloride	Others	Others
Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.

HY-15452B

Selisistat R-enantiomer EX-527 (R-enantiomer)	Sirtuin	Cancer
Selisistat R-enantiomer (EX-527 R-enantiomer) is much less active R-enantiomer of Selisistat, with an IC₅₀ of > 100 μM for SIRT1.

HY-13038B

Fostamatinib disodium hexahydrate R788 disodium hexahydrate	Syk	Inflammation/Immunology
Fostamatinib disodium hexahydrate (R788 disodium hexahydrate), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

HY-106873

Nepinalone
Others Others

Nepinalone, an alchilaminate derivative of β-tetralone and an orally active cough suppressant, possesses a non-opioid antitussive activity.

HY-15781A

Morinidazole (R enantiomer) R-Morinidazole	Bacterial	Infection
Morinidazole R enantiomer is the R-enantiomer of Morinidazole. Morinidazole is a new 5-nitroimidazole class antimicrobial agent. Morinidazole R enantiomer is the less active enantiomer.

HY-U00049

Mioflazine	Others	Neurological Disease Cardiovascular Disease
Mioflazine is an orally active nucleoside transport inhibitor, has the potential for sleep disorders treatment. Mioflazine inhibits nucleoside uptake.

HY-B1682

Loracarbef
Antibiotic Bacterial Infection

Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.

HY-N0214

Peimisine Ebeiensine	Others	Others
Peimisine(Ebeiensine) is a steroidal alkaloid which is the major biologically active component in Bulbus Fritillariae; possess a variety of toxicological and pharmacological effects on humans.

HY-101565

AMG-176
Bcl-2 Family Cancer

AMG-176 is a potent, selective and orally active MCL-1 inhibitor, with a K_i of 0.13 nM.
HY-50295

CI-1040
PD 184352
MEK Apoptosis Cancer

CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC₅₀ of 17 nM for MEK1.
HY-U00031

Axomadol
EN3324
Others Neurological Disease

Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines.

HY-N0661

Alliin	Others	Inflammation/Immunology Cardiovascular Disease
Alliin, an orally active sulfoxide compound derived from garlic, exhibits hypoglycemic, antioxidant and anti-inflammatory activities.

HY-15295

Vonoprazan Fumarate TAK-438	Proton Pump	Endocrinology
Vonoprazan Fumarate (TAK-438) is an orally active potassium-competitive acid blocker which inhibits H⁺, K⁺-ATPase activity with an IC₅₀ of 19 nM.

HY-100651

Desmethylnortriptyline	Drug Metabolite	Neurological Disease
Desmethylnortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.

HY-B2111

(R)-(+)-Atenolol
Adrenergic Receptor Others

(R)-(+)-Atenolol is the less active enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a β-adrenergic receptor antagonist.

HY-109001

Alicapistat ABT-957	Proteasome	Neurological Disease
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).

HY-109057

Enarodustat JTZ-951	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC₅₀ of 0.22 μM. Enarodustat has the potential for renal anemia treatment.

HY-Y0272

Saccharin
Bacterial Inflammation/Immunology

Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.

HY-10888

Istradefylline KW-6002	Adenosine Receptor	Neurological Disease
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with K_i of 2.2 nM in experimental models of Parkinson's disease.

HY-B1682A

Loracarbef hydrate	Antibiotic Bacterial	Infection
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.

HY-40354B

(3S,4R)-Tofacitinib
JAK Inflammation/Immunology

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-106873A

Nepinalone hydrochloride	Others	Others
Nepinalone hydrochloride, an alchilaminate derivative of β-tetralone and an orally active cough suppressant, possesses a non-opioid antitussive activity.

HY-100087

Budesonide impurity C	Glucocorticoid Receptor	Cancer Inflammation/Immunology
Budesonide impurity C is an impurity of Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist.

HY-101790A

ZM223 hydrochloride	NEDD8-activating Enzyme	Cancer
ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.

HY-40354D

(3R,4S)-Tofacitinib
JAK Inflammation/Immunology

(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-14789

(R)-Elagolix NBI-56418	GNRH Receptor	Cancer Endocrinology
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).

HY-136109

SEP-363856 hydrochloride SEP-856 hydrochloride	5-HT Receptor	Neurological Disease
SEP-363856 hydrochloride（SEP-856 hydrochloride）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride（SEP-856 hydrochloride） has the potential for the treatment of schizophrenia.

HY-B0602

Desvenlafaxine O-Desmethylvenlafaxine	Serotonin Transporter	Neurological Disease
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC₅₀ values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.

HY-101813

Laflunimus HR325	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Prostaglandin Receptor	Inflammation/Immunology
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC₅₀ values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.

HY-100740

Lanabecestat AZD3293; LY3314814	Beta-secretase	Neurological Disease
Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a K_i of 0.4 nM.

HY-112633

SMN-C3
DNA/RNA Synthesis Others

SMN-C3 is an orally active SMN2 splicing modulator and has the potential to treat spinal muscular atrophy (SMA).
HY-15157

Calcitetrol
1α, 24, 25-Trihydroxy VD3
VD/VDR Metabolic Disease

Calcitetrol(1α, 24, 25-Trihydroxy VD3) is the hormonally active form of vitamin D with three hydroxyl groups.

HY-14855A

(S)-Tedizolid (S)-TR 700; (S)-DA 7157	Others	Infection
(S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer.

HY-112218A

(R)-MIK665
Bcl-2 Family Cancer

(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC₅₀ of 1.81 nM.
HY-19727

FOY 251 free base
Others Metabolic Disease

FOY 251 free base is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.

HY-107494A

all-trans-4-Oxoretinoic acid all-trans 4-Keto Retinoic Acid	Endogenous Metabolite	Metabolic Disease
all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).

HY-12785

Albendazole sulfoxide Ricobendazole; Albendazole oxide	Parasite	Infection
Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes.

HY-14936

Sofigatran MCC-977	Thrombin	Cardiovascular Disease
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease.

HY-125826

Heptasaccharide Glc4Xyl3		Metabolic Disease
Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature.

HY-19427A

AZD9056 hydrochloride	P2X Receptor	Inflammation/Immunology
AZD9056 hydrochloride is a selective orally active inhibitor of *P2X7* which plays a significant role in inflammation and pain-causing diseases.

HY-B0378A

Moexipril hydrochloride RS-10085	Angiotensin-converting Enzyme (ACE) Apoptosis	Cardiovascular Disease
Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure.

HY-10569

Ponesimod
ACT-128800
LPL Receptor Inflammation/Immunology

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.

HY-P0206

Bradykinin	Bradykinin Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
Bradykinin is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions.

HY-B0996

Hexetidine NSC-17764	Bacterial Fungal	Infection
Hexetidine is an orally active antiseptic with broad antibacterial and antifungal activity. Hexetidine give important potential for treatment of oral infections.

HY-10212

BIIB021
CNF2024
HSP Autophagy Cancer

BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a K_i and an EC₅₀ of 1.7 nM and 38 nM, respectively.

HY-N5120

Dihydrowithaferin A 2,3-Dihydrowithaferin A	AChE	Cancer
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE).

HY-10502A

Tipifarnib S enantiomer (S)-(-)-R-115777; IND-58359 S enantiomer	Farnesyl Transferase	Cancer
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC₅₀ of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.

HY-107456

E6130
Others Inflammation/Immunology Endocrinology

E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.

HY-13728B

(Rac)-Plevitrexed (Rac)-ZD 9331; (Rac)-BGC9331	Thymidylate Synthase	Cancer
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331) is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.

HY-111494

TRPA1 Antagonist 1	TRP Channel	Neurological Disease
TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC₅₀ of 8 nM.

HY-N7500

Ginsenoside Rh8	Others	Inflammation/Immunology
Ginsenoside Rh8 is a saponin composition of roots of Panax ginseng. Ginsenosides are the major active pharmacological components of ginseng.

HY-12772

Hydroxy Itraconazole Itraconazole metabolite Hydroxy Itraconazole; R-63373	Fungal Drug Metabolite	Others
Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

HY-100744

AS8351 NSC51355	Histone Demethylase	Cardiovascular Disease
AS8351 is a KDM5B inhibitor, which can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells.

HY-13464

ALK-IN-1
Brigatinib analog
ALK Cancer

ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

HY-B0806

Proguanil	Parasite Antifolate	Infection
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.

HY-B0975

Penicillin V Potassium Phenoxymethylpenicillin potassium salt	Bacterial Antibiotic	Infection
Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an antibiotic useful for the treatment of a number of bacterial infections, is a penicillin that is orally active, acts by inhibiting the biosynthesis of cell-wall peptidoglycan.

HY-107496

Imidocarb dipropionate	Parasite Antibiotic	Infection
Imidocarb dipropionate is a potent antiprotozoal agent. Imidocarb dipropionate is active against the parasite B. bovis with an IC₅₀ of 87 μg/mL.

HY-101833

YM-264
Others Inflammation/Immunology

YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.

HY-B0806A

Proguanil hydrochloride	Parasite Antifolate	Infection
Proguanil hydrochloride, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.

HY-40354C

(3S,4S)-Tofacitinib
JAK Inflammation/Immunology

(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-15853A

MK-7246 S enantiomer	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
MK-7246 S enantiomer is the less active enantiomer of MK-7246. MK-7246 is a potent and selective CRTH2 antagonist.

HY-17646

Verdiperstat AZD3241	Glutathione Peroxidase	Neurological Disease
Verdiperstat (AZD3241) is a selective, irreversible and orally active myeloperoxidase (MPO) inhibitor, with an IC₅₀ of 630 nM, and can be used in the research of neurodegenerative brain disorders.

HY-30272

Monobenzone	Others	Inflammation/Immunology
Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and active human vitiligo and exhibits good potential for vitiligo research.

HY-N0892

AKBA Acetyl-11-keto-β-boswellic acid	HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Endogenous Metabolite	Cancer
AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.

HY-70002AS

N-desmethyl Enzalutamide D6 N-desmethyl MDV 3100 D6	Androgen Receptor	Cancer
N-desmethyl Enzalutamide D6 (N-desmethyl MDV 3100 D6) is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide.

HY-133781S

cis-Clopidogrel-MP Derivative 13CD3 Clopidogrel-MP-AM 13CD3	Others	Others
cis-Clopidogrel-MP Derivative 13CD3 (Clopidogrel-MP-AM 13CD3) is a deuterium labele cis-Clopidogrel-MP Derivative. cis-Clopidogrel-MP Derivative is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor.

HY-B0602A

Desvenlafaxine succinate hydrate O-Desmethylvenlafaxine succinate hydrate	Serotonin Transporter	Neurological Disease
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC₅₀ values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.

HY-A0279

Pristinamycin Pristinamycine	Bacterial	Infection
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF).

HY-135334

ACP-5862	Drug Metabolite Btk Cytochrome P450	Cancer
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC₅₀ of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of *CYP3A4* and *CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC₅₀ of 3 nM and EC₅₀ of 8 nM.*

HY-15848

AdipoRon	Adiponectin Receptor	Metabolic Disease
AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with K_ds of 1.8 and 3.1 μM, respectively.

HY-13256

Desmethyl Erlotinib OSI-420; CP-473420	Drug Metabolite	Cancer
Desmethyl Erlotinib (OSI-420; CP-473420) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.

HY-101570A

(R)-Nedisertib
(R)-M3814
DNA-PK Cancer

(R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC₅₀ in the range of 7-30 nM for DNA-PK.

HY-50714

Quiflapon sodium MK-591 sodium	FLAP Apoptosis	Inflammation/Immunology
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.

HY-109592

Imidaprilate 6366A; Imidaprilat	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC₅₀ of 2.6 nM, and is used in the research of hypertensive disease.

HY-110164

AdipoRon hydrochloride	Adiponectin Receptor	Metabolic Disease
AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM, respectively.

HY-B0196A

Venlafaxine hydrochloride Wy 45030 hydrochloride	Serotonin Transporter	Neurological Disease
Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.

HY-14719

RO4987655
CH4987655
MEK Cancer

RO4987655 is an orally active and highly selective MEK inhibitor with an IC₅₀ of 5.2 nM for inhibition of MEK1/MEK2.
HY-114272A

T4-ATA (S-isomer)
Thyroid Hormone Receptor Endocrinology

T4-ATA S-isomer is the S-isomer of T4-ATA, which is the active form of the thyroid hormone.
HY-18030A

CEP-28122 mesylate salt
ALK Cancer

CEP-28122 mesylate salt is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
HY-119217

AZ084
CCR Inflammation/Immunology Endocrinology

AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a K_i of 0.9 nM. Has potential to treat asthma.
HY-19778

(R)-BPO-27
CFTR Autophagy Inflammation/Immunology

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC₅₀ of 4 nM.
HY-112895A

(R)-UT-155
Androgen Receptor Cancer

(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.

HY-122924

Theogallin 3-Galloylquinic acid	Others	Neurological Disease
Theogallin (3-Galloylquinic acid) is an active ingredient in decaffeinated green tea extract. Theogallin has antidepressive and cognition enhancing effect.

HY-133740

MS117
Histone Methyltransferase Cancer

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC₅₀ of 18 nM.
HY-114271A

T3-ATA (S-isomer)
Thyroid Hormone Receptor Endocrinology

T3-ATA S-isomer is the S-isomer of T3-ATA, which is the active form of the thyroid hormone.
HY-111802

3,4'-Dihydroxyflavone
3,4'-DHF
Influenza Virus Infection

3,4'-Dihydroxyflavone (3,4'-DHF) is an oral active flavonoid with antiviral activity against Influenza A virus.
HY-101114

LAS191954
PI3K Inflammation/Immunology

LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC₅₀ of 2.6 nM.

HY-100007

Vonoprazan TAK-438 free base	Proton Pump	Endocrinology
Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H⁺, K⁺-ATPase activity with an IC₅₀ of 19 nM.

HY-18030

CEP-28122
ALK Cancer

CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.

HY-B2157

Robenidine hydrochloride	Bacterial Parasite	Infection
Robenidine hydrochloride is an anticoccidial agent which is also active against MRSA and VRE with MIC₅₀s of 8.1 and 4.7 μM, respectively.

HY-B1096

Etamivan Ethamivan; N,N-Diethylvanillamide	Others	Neurological Disease
Etamivan (Ethamivan), an orally active respiratory stimulant, is mainly used in the research of barbiturate overdose and chronic obstructive pulmonary disease.

HY-129336

CDK4/6-IN-4
CDK Cancer

CDK4/6-IN-4, the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.

HY-B0196

Venlafaxine Wy 45030	Serotonin Transporter	Neurological Disease
Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.

HY-15405

Teriflunomide A77 1726	Others	Inflammation/Immunology
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.

HY-N0483

Phillygenin Phillygenol; Epipinoresinol methyl ether; (+)-Phillygenin	Reactive Oxygen Species	Others
Phillygenin (Phillygenol) is an active ingredient from Forsythia with many medicinal properties, such as antioxidant, reducing blood lipid, inhibition of low density lipoprotein oxidation.

HY-13432

Nanatinostat
CHR-3996
HDAC Cancer

Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC₅₀ of 8 nM.

HY-10159A

Nilotinib monohydrochloride monohydrate AMN107 (monohydrochloride monohydrate)	Bcr-Abl Autophagy	Cancer
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.

HY-N0465

Olaquindox	Bacterial	Infection
Olaquindox, a quinoxalin derivative, is an orally active antibiotic veterinary drug. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets.

HY-101749

WAY127093B racemate	Phosphodiesterase (PDE)	Inflammation/Immunology
WAY127093B racemate is the racemate of WAY127093B. WAY127093B is an orally active phosphodiesterase IV inhibitor in guinea pigs and rats.

HY-U00035

MGB-BP-3
Bacterial Infection

MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.

HY-12772S

Hydroxy Itraconazole D8 R-63373 D8	Fungal	Others
Hydroxy Itraconazole D8 is the deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

HY-Y1750

β-Aminopropionitrile	Monoamine Oxidase	Cancer
β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes.

HY-N1433

Phytolaccagenin	Bacterial	Infection Inflammation/Immunology
Phytolaccagenin, a triterpenoid saponin, is the active component of Radix Phytolaccae. Phytolcaccagenin has antifungal activity, anti-inflammatory activity and lower toxicity

HY-15345

Tetrahydrouridine dihydrate THU dihydrate; NSC-112907 dihydrate	Others	Cancer
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

HY-12993B

RSV604 R enantiomer	RSV	Infection
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.

HY-U00160

SP187 MON-DNJ; UV4	Influenza Virus	Infection
SP187 is a host-targeted iminosugar with activity against filovirus infections in vitro and in vivo. SP187 is active against influenza and dengue in vivo.

HY-19715

SGC707
Histone Methyltransferase Cancer

SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.

HY-14503

MDR-1339 DWK-1339	Amyloid-β	Neurological Disease
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.

HY-116830A

(Rac)-BRD0705	GSK-3	Cancer
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC₅₀ of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).

HY-107429

Abrocitinib PF-04965842	JAK	Inflammation/Immunology
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

HY-N5004

Guanfu base I Acorine	Others	Cardiovascular Disease
Guanfu base I (Acorine) is an active metabolite of Guanfu base A, isolated from Aconitum coreanum, and has a potent anti-arrhythmic effect.

HY-135391

Ezetimibe phenoxy glucuronide Ezetimibe glucuronide; Ezetimibe β-D-glucuronide	Drug Metabolite	Metabolic Disease
Ezetimibe phenoxy glucuronide (Ezetimibe glucuronide) is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.

HY-121467S

Acotiamide D6	AChE	Metabolic Disease
Acotiamide D6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia.

HY-N0006

Demethoxycurcumin Curcumin II; Desmethoxycurcumin; Monodemethoxycurcumin	Apoptosis Autophagy Bacterial	Inflammation/Immunology Cancer
Demethoxycurcumin(Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.

HY-N2909

Aurantiamide	Others	Inflammation/Immunology
Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities.

HY-19989A

MK-571 sodium salt L-660711 sodium salt	Leukotriene Receptor	Inflammation/Immunology
MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with K_is of 0.22 and 2.1 nM in guinea pig and human lung membranes.

HY-P0251

Neurotensin(8-13)	Neurotensin Receptor	Neurological Disease
Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.

HY-B1459

Dicloxacillin sodium	Bacterial Antibiotic	Infection
Dicloxacillin sodium is a narrow-spectrum β-lactam antibiotic of the penicillin family. Dicloxacillin sodium is active against β-lactamase-producing organisms such as Staphylococcus aureus.

HY-19371

Lorediplon	GABA Receptor	Neurological Disease
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.

HY-16346S

Netupitant D6 CID-6451149 D6	Neurokinin Receptor	Endocrinology Neurological Disease
Netupitant D6 is the deuterium labeled Netupitant(CID-6451149), which is a highly potent and selective, orally active neurokinin-1 receptor antagonist.

HY-N1476

Heterophyllin B	PI3K	Cancer
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.

HY-19562

PF-06260933
MAP4K Inflammation/Immunology

PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC₅₀s of 3.7 and 160 nM for kinase and cell, respectively.
HY-100694

GS-9901
PI3K Inflammation/Immunology

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC₅₀ of 1 nM. Has potential to treat rheumatoid arthritis.

HY-N5007

Galgravin	Others	Cancer
Galgravin is an active compound in Nectandra megapotamica, with anti-inflammatory activity. Galgravin displays in vitro cytotoxic activity and induce apoptosis in leukemia cells.

HY-101760

GSK2982772	RIP kinase	Inflammation/Immunology
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC₅₀ values of 16 nM and 20 nM for human and monkey RIP1, respectively.

HY-103334

MAFP Methyl Arachidonyl Fluorophosphonate	Phospholipase	Metabolic Disease Neurological Disease Cardiovascular Disease
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of *cPLA2* and *iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase*.

HY-N0159

Paeonol	Monoamine Oxidase Autophagy	Neurological Disease Cancer
Paeonol is an active extraction from the root of Paeonia suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC₅₀ of 54.6 μM and 42.5 μM, respectively.

HY-B0216

Ethynyl Estradiol 17α-Ethynylestradiol; Ethynylestradiol	Estrogen Receptor/ERR Endogenous Metabolite	Endocrinology Cancer
Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

HY-B0132A

Norfloxacin hydrochloride MK-0366 hydrochloride	Bacterial Antibiotic	Infection
Norfloxacin hydrochloride (MK-0366 hydrochloride) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.

HY-N5064

Bacoside A3
Others Neurological Disease

Bacoside A3, a triterpenoid saponin, is one of the major active constituents in Bacopa monnieri. Bacoside A3 has neuroprotective activity.

HY-19657

Oxypurinol Oxipurinol	Endogenous Metabolite Xanthine Oxidase	Metabolic Disease Inflammation/Immunology
Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout.

HY-16472

Sulfacytine	Antibiotic Bacterial	Infection
Sulfacytine is a short-acting sulfonamide antibiotic. Sulfacytine is active against bacteria and is an effective drug for the research of acute uncomplicated urinary tract infections.

HY-B0132

Norfloxacin MK-0366	Bacterial Endogenous Metabolite Antibiotic	Infection
Norfloxacin (MK-0366) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.

HY-19214

Elisartan HN 65021	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Elisartan is an orally active non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.

HY-135601

Cinacalcet metabolite M4	Drug Metabolite	Cardiovascular Disease
Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease.

HY-50949A

Bay 65-1942 R form
IKK Inflammation/Immunology

Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.

HY-124557

Mahanimbine	Others	Metabolic Disease Inflammation/Immunology
Mahanimbine is an orally active alkaloid from curry leaves. Mahanimbine inhibits progression of high-fat diet (HFD)-induced metabolic complications in mice.

HY-128449

Cephradine monohydrate Cefradine monohydrate	Bacterial Antibiotic	Infection
Cephradine monohydrate (Cefradine monohydrate) is a first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria.

HY-N0253

Hederacoside C Kalopanaxsaponin B	Bacterial	Infection
Hederacoside C is a principal active ingredient of Hedera helix leaf that can treat respiratory disorders, because of its expectorant, bronchodilator, antibacterial, and bronchospasmolytic effects.

HY-10454

Delanzomib CEP-18770	Proteasome	Cancer
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.

HY-17608

Daprodustat GSK1278863	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

HY-N0784

Ginkgolide B BN-52021	Endogenous Metabolite	Cancer
Ginkgolide B (BN-52021), an important active terpenoid from Ginkgo biloba leaves, is reported to increase cell viability and decrease cell apoptosis.

HY-B0610

Misoprostol
SC-29333
Prostaglandin Receptor Endocrinology

Misoprostol (SC-29333) is an orally active synthetic prostaglandin E1 (PGE1) analog that is used for gastric ulcers research.

HY-101857

MGAT2-IN-1	Acyltransferase	Metabolic Disease
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC₅₀ of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

HY-12449

Crenigacestat
LY3039478
Notch γ-secretase Cancer

Crenigacestat is an orally active Notch and γ-secretase inhibitor, with an IC₅₀ of ∼1nM in most of the tumor cell lines tested.

HY-136109B

(Rac)-SEP-363856 (Rac)-SEP-856	5-HT Receptor	Neurological Disease
(Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856（SEP-856）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 （SEP-856） has the potential for the treatment of schizophrenia.

HY-N6022

Byakangelicin	Others	Metabolic Disease
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.

HY-100720

GSK2193874
TRP Channel Cardiovascular Disease

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC₅₀s of 2 nM and 40 nM for rTRPV4 and hTRPV4.

HY-112790

Adenosylcobalamin Coenzyme B12; Cobamamide; AdoCbl	Endogenous Metabolite	Metabolic Disease
Adenosylcobalamin (Coenzyme B12;Cobamamide;AdoCbl) is an active form of Vitamin B₁₂ which is a cofactor for methylmalonyl CoA mutase

HY-100069

Fluazinam impurity 1	Fungal	Infection
Fluazinam impurity 1 is an impurity of Fluazinam with antifungal activity. Fluazinam impurity 1 is active against *Sphaerotheca fuliginea, Pyricularia oryzae* and *Rhizoctonia solani*.

HY-A0068

Aurothioglucose Gold thioglucose	Others	Cancer
Aurothioglucose (Gold thioglucose) is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.

HY-B0106A

Etiracetam UCB 6474	Calcium Channel	Neurological Disease
Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059).

HY-32709

Telcagepant MK-0974	CGRP Receptor	Neurological Disease
Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with K_is of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

HY-N0227

7-epi-Taxol 7-epi-Paclitaxel	Microtubule/Tubulin	Cancer
7-epi-Taxol is an active metabolite of taxol, with activity comparable to that of taxol against cell replication, promoting microtubule bundle formation and against microtubule depolymerization.

HY-14880B

Bavisant dihydrochloride hydrate JNJ31001074AAC	Histamine Receptor	Neurological Disease Endocrinology
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

HY-B0524A

Betahistine dihydrochloride	Histamine Receptor	Endocrinology Inflammation/Immunology Neurological Disease
Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).

HY-118930

MK-0493	Melanocortin Receptor	Endocrinology Metabolic Disease
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.

HY-107833

A40926	Bacterial	Infection
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae.

HY-B0978

Diethyltoluamide DEET; N,N-Diethyl-m-toluamide	Parasite	Infection
Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects.

HY-117771

DO34	Others	Metabolic Disease
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC₅₀ of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC₅₀ for DAGLβ.

HY-I0021

Bepotastine	Histamine Receptor	Endocrinology Inflammation/Immunology
Bepotastine is an orally active second-generation histamine H1 receptor antagonist. Bepotastine has the potential for allergic rhinitis and urticaria/pruritus treatment.

HY-12481A

SAR405 R enantiomer
Others Cancer

SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.

HY-A0100

Thiamine monochloride Vitamin B1	Others	Metabolic Disease Neurological Disease
Thiamine monochloride (Vitamin B1) is an essential vitamin that plays an important role in cellular production of energy from ingested food and enhances normal neuronal actives.

HY-18632

GSK2879552	Histone Demethylase	Cancer
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.

HY-100015

Mivebresib ABBV-075	Epigenetic Reader Domain Apoptosis	Cancer
Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K_i of 1.5 nM.

HY-14615

[6]-Gingerol (S)-(+)-[6]Gingerol; 6-Gingerol	AMPK Apoptosis	Cancer
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.

HY-112445

SGC3027
Histone Methyltransferase Cancer

SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.

HY-125465

SLLN-15	Autophagy	Cancer
SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).

HY-W013172

Norgestimate	Progesterone Receptor	Endocrinology
Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive.

HY-14781

Levomefolic acid 5-MTHF	Endogenous Metabolite Reactive Oxygen Species	Cancer
Levomefolic acid (5-MTHF) is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.

HY-Y1903

Phosal 50 PG	Others	Others
Phosal 50 PG is a standardized phosphatidylcholine concentrate, used in some lipid-based formulations to improve the absorption, effectiveness, and therapeutic index of the active ingredients.

HY-14880

Bavisant JNJ-31001074	Histamine Receptor	Neurological Disease Endocrinology
Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

HY-B0524

Betahistine	Histamine Receptor	Cancer Inflammation/Immunology
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).

HY-11029

SNT-207707	Melanocortin Receptor	Cancer Metabolic Disease Endocrinology
SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC₅₀ of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.

HY-101281B

(R)-VU 6008667
Others Neurological Disease

(R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC₅₀>10 μM).
HY-12422B

(2S,3R)-Voruciclib hydrochloride
CDK Cancer

(2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. (2S,3R)-Voruciclib is an orally active CDK inhibitor.

HY-19947

PF-06291874 Glucagon receptor antagonists-4	Glucagon Receptor	Metabolic Disease
PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs.

HY-N6666

Vidarabine monohydrate	HSV Antibiotic	Infection
Vidarabine monohydrate is an adenine arabinoside. Vidarabine monohydrate an antiviral drug which is active against herpes simplex viruses (HSV) and varicella zoster viruses.

HY-101265

S1p receptor agonist 1	LPL Receptor	Inflammation/Immunology
S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC₅₀=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.

HY-109010

Poseltinib HM71224; LY3337641	Btk BMX Kinase Toll-like Receptor (TLR)	Metabolic Disease
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC₅₀ =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.

HY-B1454

Clindamycin palmitate hydrochloride	Bacterial Antibiotic	Infection
Clindamycin palmitate hydrochloride is a water soluble hydrochloride salt of the ester of clindamycin and palmitic acid and it is an antibacterial drug. Clindamycin palmitate hydrochloride is inactive in vitro, rapid in vivo hydrolysis converts this compound to the antibacterially active clindamycin.

HY-U00179

CDC801	Phosphodiesterase (PDE) TNF Receptor	Cancer
CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC₅₀ of 1.1 μM and 2.5 μM, respectively.

HY-12305A

(R)-Q-VD-OPh (R)-QVD-OPH; (R)-Quinoline-Val-Asp-Difluorophenoxymethylketone	Others	Cancer
(R)-Q-VD-OPh ((R)-QVD-OPH) is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible pan-caspase inhibitor with potent antiapoptotic properties.

HY-B0804S

Nadolol D9 SQ-11725 D9	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Nadolol D9 (SQ-11725 D9) is the deuterium labeled Nadolol. Nadolol is a non-selective and orally active β-adrenergic receptors blocker.

HY-13660

Mocravimod hydrochloride KRP-203	LPL Receptor	Inflammation/Immunology
Mocravimod hydrochloride (KRP-203), an immunosuppressant, is a potent and orally active S1PR1 (sphingosine 1-phosphate receptor type 1) agonist.

HY-14880A

Bavisant dihydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Bavisant Hcl (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

HY-15005B

Sofosbuvir impurity C	Others	Others
Sofosbuvir impurity C is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-123046

AS1708727
Others Cancer Metabolic Disease

AS1708727 is an orally active Foxo1 inhibitor, with EC₅₀ values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.

HY-101023

MK-8617	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC₅₀ of 1 nM for *PHD2*.

HY-115506

PF-05105679
TRP Channel Neurological Disease

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC₅₀ of 103 nM. PF-05105679 has the potential for cold-related pain.

HY-N0804

Narirutin	Bacterial	Inflammation/Immunology
Narirutin, one of the active constituents isolated from Citrus unshiu, has antioxidant and anti-inflammatory activities. Narirutin is a shikimate kinase inhibitor with anti-tubercular potency.

HY-101873

Atorvastatin lactone	HMG-CoA Reductase (HMGCR)	Metabolic Disease Inflammation/Immunology
Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.

HY-N0300

Tetrahydropalmatine DL-Tetrahydropalmatine	Dopamine Receptor Apoptosis	Neurological Disease
Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.

HY-129405

N-(Ketocaproyl)-D,L-homoserine lactone	Bacterial	Infection
N-(Ketocaproyl)-D,L-homoserine lactone is a natural, very active ligand of LuxR. N-(Ketocaproyl)-D,L-homoserine lactone is a quorum sensing (QS) autoinducer.

HY-I0727

Sofosbuvir impurity E	Others	Others
Sofosbuvir impurity E is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-10402

Losmapimod GSK-AHAB; GW856553X; SB856553	p38 MAPK Autophagy	Inflammation/Immunology Cancer
Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pK_is of 8.1 and 7.6 for p38α and p38β, respectively.

HY-N0557

Isoescin IB
Others Cancer

Isoescin IB, isolated from horse chestnut tree seeds, is an isomer of Escin IB. Isoescin IB and Escin IB are the chief active ingredients in escin.

HY-109136

Runcaciguat	Guanylate Cyclase	Cardiovascular Disease
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.

HY-15123

(S)-Flurbiprofen Esflurbiprofen	COX PGE synthase	Inflammation/Immunology
(S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC₅₀ values of 0.48 μM and 0.47 μM for COX-1 and *COX-2*, respectively.

HY-108717

Protease K	Others	Others
Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures.

HY-N0248

Saikosaponin B2
HCV Cancer Infection

Saikosaponin B2 is an active component from Bupleurum kaoi root, acts as an entry inhibitor against HCV infection. Anti-cancer activity.

HY-114192

TGFβRI-IN-1	TGF-β Receptor	Cancer
TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC₅₀ values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .

HY-U00333

α1 adrenoceptor-MO-1	Adrenergic Receptor	Neurological Disease Endocrinology
α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.

HY-101069

Y-26763
Potassium Channel Cardiovascular Disease

Y-26763 is a K⁺ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K⁺ (K_ATP) channel activator.

HY-18715

Ornidazole (Levo-) (S)-Ornidazole; Levornidazole	Bacterial Parasite	Infection
Ornidazole Levo- is the levo-isomer of Ornidazole. Ornidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Ornidazole Levo- is the less active isomer.

HY-100646A

(Z)-10-Hydroxy Nortriptyline	Drug Metabolite	Neurological Disease
(Z)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.

HY-101125

L-45
L-Moses
Epigenetic Reader Domain Cancer

L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a K_d of 126±15 nM.
HY-N2487

5-Hydroxy-7-acetoxyflavone
Others Cancer

5-Hydroxy-7-acetoxyflavone, an active natural flavone derivative found in various plant sources, modulates several biological activities.
HY-101907

ASP7663
TRP Channel Neurological Disease

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.

HY-15614A

SC144 hydrochloride	Interleukin Related	Cancer
SC144 hydrochloride is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.

HY-W074930

(S)-Tenofovir (S)-GS 1278; (S)-PMPA; (S)-TDF	HIV HBV	Infection
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).

HY-102087

JPM-OEt	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.

HY-I0719

Sofosbuvir impurity B	Others	Others
Sofosbuvir impurity B is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-B1695

Methyl nicotinate	Others	Inflammation/Immunology
Methyl nicotinate, the methyl ester of Niacin found in alcoholic beverages, that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain.

HY-14616

Shogaol [6]-Shogaol; 6-Shogaol	Autophagy	Cancer
Shogaol ([6]-Shogaol), an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.

HY-103081

β-Glucuronidase-IN-1	Bacterial	Cancer Infection
β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC₅₀ and a K_i of 283 nM and 164 nM, respectively.

HY-15614

SC144	Interleukin Related	Cancer
SC144 is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.

HY-30152

Xanthotoxol 8-Hydroxypsoralen	5-HT Receptor Reactive Oxygen Species Endogenous Metabolite	Inflammation/Immunology Neurological Disease
Xanthotoxol (8-Hydroxypsoralen) is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.

HY-15283

Clopidogrel	P2Y Receptor	Cardiovascular Disease
Clopidogrel is an orally active platelet inhibitor that targets *P2Y12* receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.

HY-107575

TLR4-IN-C34	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

HY-128599

NMS-P515
PARP Cancer

NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a K_d of 16 nM and an IC₅₀ of 27 nM (in Hela cells). Anti-tumor activity.

HY-12469

Decernotinib VX-509; VRT-831509	JAK	Inflammation/Immunology
Decernotinib is a potent, orally active *JAK3* inhibitor, with K_is of 2.5, 11, 13 and 11 nM for *JAK3*, JAK1, JAK2, and TYK2, respectively.

HY-13990

NVP-TNKS656 TNKS656	PARP Apoptosis	Cancer
NVP-TNKS656 is a highly potent, selective, and orally active *TNKS2* inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and *PARP2*.

HY-101363

1-BCP Piperonylic acid piperidide	iGluR	Neurological Disease
1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.

HY-I0723

Sofosbuvir impurity D	Others	Others
Sofosbuvir impurity D is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-135013

Umbellulone	TRP Channel	Neurological Disease
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

HY-12472

Balipodect TAK-063	Phosphodiesterase (PDE)	Neurological Disease
Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC₅₀ of 0.30 nM; >15000-fold selectivity over other PDEs.

HY-136346

2-Hydroxy atorvastatin lactone	Drug Metabolite	Others
2-Hydroxy atorvastatin lactone is a metabolite of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.

HY-100646

(E)-10-Hydroxy Nortriptyline maleate	Drug Metabolite	Neurological Disease
(E)-10-Hydroxy Nortriptyline maleate is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.

HY-100316

CP-96486	Leukotriene Receptor	Inflammation/Immunology
CP-96486 is a potent and orally active leukotriene D₄ (LTD₄)/platelet activating factor (PAF) receptor antagonist with K_is of 20 and 24 nM, respectively.

HY-12835

S1P1 Agonist III
LPL Receptor Inflammation/Immunology

S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.
HY-13469

Debio 0932
CUDC-305
HSP Cancer

Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC₅₀s of 100 and 103 nM for HSP90α and HSP90β, respectively.

HY-W006405

Isoflavone	Others	Others
Isoflavone, a soy phytoestrogen and a biologically active component, presents in several agriculturally important legumes such as soy, peanut, green peas, chick peas and alfalfa.

HY-10333

BMS-690514	EGFR VEGFR	Cardiovascular Disease Cancer
BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

HY-123076

Pifithrin-α, p-Nitro, Cyclic PFN-α	MDM-2/p53	Neurological Disease
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED₅₀=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.

HY-101561

Avapritinib BLU-285	c-Kit PDGFR	Cancer
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.

HY-119580

Leucocyanidin	Others	Inflammation/Immunology
Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from unripe plantain banana. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models.

HY-101509

HSL-IN-1	Others	Metabolic Disease
HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC₅₀=2 nM) with a significantly reduced reactive metabolite liability.

HY-P0184

Camstatin
NO Synthase Neurological Disease

Camstatin, a functionally active 25-residue fragment of PEP-19's IQ motif, binds calmodulin and inhibits neuronal nitric oxide (NO) synthase.
HY-101783

GNE-955
Pim Cancer

GNE-955 is a potent and orally active pan Pim kinase inhibitor with K_is of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
HY-B0790

TAI-1
Apoptosis Cancer

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI₅₀ of 13.48 nM in K562 cells.

HY-B1651

Iron(II) fumarate Ferrous fumarate	Others	Metabolic Disease
Iron(II) fumarate (Ferrous fumarate) is the iron(II) salt of fumaric acid. Iron(II) fumarate is an orally active dietary supplement and has the potential for iron deficiency anemia treatment.

HY-N6020

(-)-Butin	Others	Inflammation/Immunology
(-)-Butin is the S enantiomer of Butin. Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities.

HY-13636B

Fulvestrant (R enantiomer) ICI 182780 (R enantiomer); ZD 9238 (R enantiomer); ZM 182780 (R enantiomer)	Others	Cancer
Fulvestrant R enantiomer (ICI 182780 R enantiomer; ZD 9238 R enantiomer; ZM 182780 R enantiomer) is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC₅₀ of 9.4 nM.

HY-15600

UPF-648	Others	Neurological Disease
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.

HY-N0692

Schisandrol B Gomisin-A; TJN-101; Wuweizi alcohol-B	Autophagy	Cancer
Schisandrol B (Gomisin-A;TJN-101;Wuweizi alcohol-B) is one of its major active constituents of traditional hepato-protective Chinese medicine, Schisandra sphenanthera.

HY-A0086

Netilmicin sulfate SCH-20569 sulfate	Bacterial Antibiotic	Infection
Netilmicin (sulfate) (SCH-20569 (sulfate)) is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.

HY-14841

Gisadenafil UK-369003	Phosphodiesterase (PDE)	Neurological Disease
Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

HY-114162A

VTP50469 fumarate	Epigenetic Reader Domain Apoptosis	Cancer
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.

HY-107366

SGN-2FF
Others Cancer

SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.
HY-100411

MLi-2
LRRK2 Neurological Disease

MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC₅₀ of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.

HY-14365

TC-G 1004	Adenosine Receptor	Neurological Disease
TC-G 1004 (compound 16j) is an orally active A_2A adenosine receptor antagonist, with K_i values of 0.44 nM and 80 nM for hA_2A and hA₁, respectively.

HY-135381

3-Oxo Atorvastatin	Others	Cardiovascular Disease
3-Oxo Atorvastatin is an impurity of 3-Oxo Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

HY-A0015

Bepotastine (Beslilate)	Histamine Receptor	Inflammation/Immunology Endocrinology
Bepotastine Beslilate is an orally active second-generation histamine H1 receptor antagonist. Bepotastine Beslilate has the potential for allergic rhinitis and urticaria/pruritus treatment.

HY-100339

GSK583	RIP kinase	Endocrinology
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC₅₀ of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC₅₀ value of 200 nM.

HY-126131

anti-TB agent 1
Bacterial Infection

anti-TB agent 1 is a potent and orally active anti-tuberculosis agent, with MICs of < 2 nM against the Mtb strains H37Rv, rRMP and rINH.

HY-N2199

Sotetsuflavone	Others	Cancer
Sotetsuflavone is a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase) with an IC50 of 0.16 uM, is the most active compound of this series .

HY-14617

Paradol [6]-Gingerone; [6]-Paradol	COX	Cancer
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.

HY-112723

ACT-709478	Calcium Channel	Neurological Disease
ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.

HY-15600B

UPF-648 sodium salt	Others	Neurological Disease
UPF-648 sodium salt is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.

HY-128356

SPL-410	Others	Inflammation/Immunology
SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC₅₀ of 9 nM.

HY-114162

VTP50469	Epigenetic Reader Domain Apoptosis	Cancer
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 has potently anti-leukemia activity.

HY-18233

E1210 APX001A	Fungal	Infection
E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.

HY-128878

Dexloxiglumide	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).

HY-108045

Lodenafil carbonate	Phosphodiesterase (PDE)	Endocrinology
Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).

HY-B0196B

(S)-Venlafaxine	Serotonin Transporter	Cancer
(S)-Venlafaxine is the (S)-configuration of Venlafaxine. Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant agent.

HY-12480

Lanopepden GSK 1322322	Bacterial	Infection
Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively.

HY-101040

Q203 IAP6; Telacebec	Bacterial	Infection
Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC₅₀ of 2.7 nM in culture broth medium.

HY-101978

CPI-444 V81444; ciforadenant	Adenosine Receptor	Cancer
CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.

HY-14554

LY2140023	mGluR	Neurological Disease
LY2140023 is an orally active prodrug of LY404039. LY404039 is a selective metabotropic glutamate 2/3 receptor agonist. LY2140023 has the potential for schizophrenia.

HY-15675

AZD1656	Glucokinase	Metabolic Disease
AZD1656 is a potent, selective and orally active glucokinase activator with an EC₅₀ of 60 nM. AZD1656 has the potential for type 2 diabetes research.

HY-N6729

HT-2 Toxin
Others Metabolic Disease

HT-2 Toxin is an active, deacetylated metabolite of the T-2 toxin. HT-2 toxin inhibits protein synthesis and cell proliferation in plants.

HY-14925

Lapaquistat T-91485	Endogenous Metabolite	Metabolic Disease
Lapaquistat (T-91485), a cholesterol biosynthesis inhibitor, is the active metabolite of TAK-475. Lapaquistat can decrease statin-induced myotoxicity in lipid-lowering therapy.

HY-18341

L-Thyroxine Levothyroxine; T4	Thyroid Hormone Receptor Endogenous Metabolite	Endocrinology
L-Thyroxine (Levothyroxine; T4) is a synthetic hormone in the treatment of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).

HY-106147

Frakefamide	Opioid Receptor	Neurological Disease
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

HY-10806

SB-649868 GSK649868	Orexin Receptor (OX Receptor)	Metabolic Disease Endocrinology
SB-649868 is a potent and selective orally active orexin (OX) 1 and *OX₂* receptor antagonist (pK_i =9.4 and 9.5 at the OX₁ and OX₂ receptor, respectively).

HY-U00417

ARS-1630
Ras Cancer

ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.

HY-121450

Lavoltidine Loxtidine; AH-234844	Histamine Receptor	Cancer
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.

HY-10017

SCH 546738	CXCR	Inflammation/Immunology Endocrinology
SCH 546738 is a potent, orally active and non-competitive *CXCR3* antagonist, the affinity constant (K_i) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.

HY-A0279A

Pristinamycin IA Mikamycin B; Mikamycin IA	Bacterial	Others
Pristinamycin IA (Mikamycin B;Mikamycin IA), a biologically active decapeptide isolated from the skin of the Australian frog Hyla caerulea, is a potent cholecystokinetic agent, and acts as a cholecystokinin receptor agonist.

HY-B1271

Sulfinpyrazone G-28315	Others	Inflammation/Immunology
Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects.

HY-13636A

Fulvestrant (S enantiomer) ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)	Others	Cancer
Fulvestrant S enantiomer (ICI 182780 S enantiomer; ZD 9238 S enantiomer; ZM 182780 S enantiomer) is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC₅₀ of 9.4 nM.

HY-103591

DUPA(OtBu)-OH	Others	Cancer
DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

HY-14945

Remogliflozin etabonate GSK189075	SGLT	Metabolic Disease
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with K_i values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

HY-136576

RP101075	LPL Receptor Drug Metabolite	Inflammation/Immunology
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC₅₀ of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC₅₀=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.

HY-N0751

Scutellarin	STAT Akt HIV	Cancer Infection
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the *STAT3/Girdin/Akt* signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC₅₀s of 26 μM, 253 μM and 136 μM, respectively.

HY-118304

AKN-028
FLT3 Caspase Cancer

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC₅₀ = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

HY-10527

Telatinib Bay 57-9352	c-Kit PDGFR VEGFR	Cancer
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of *VEGFR2, VEGFR3, PDGFα, and c-Kit* with IC₅₀s of 6, 4, 15 and 1 nM, respectively.

HY-19456

SSR-241586	Neurokinin Receptor	Neurological Disease Endocrinology
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).

HY-125997

BTK inhibitor 10	Btk	Inflammation/Immunology
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.

HY-N0300A

Tetrahydropalmatine hydrochloride DL-Tetrahydropalmatine hydrochloride	Dopamine Receptor	Neurological Disease
Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.

HY-102036

G-744	Btk	Inflammation/Immunology
G-744 is a highly potent, selective and orally active Btk inhibitor with an IC₅₀ of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.

HY-107702

CGP 37849	iGluR	Neurological Disease
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects.

HY-100659

PCI-45227
Btk Cancer

PCI-45227 is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib.

HY-66011A

Moxifloxacin	Bacterial Antibiotic	Infection
Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.

HY-13258A

NVP-BHG712
BHG712
Ephrin Receptor Cancer

NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC₅₀ values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively.

HY-103252

Monomethyl fumarate	GPR109A Drug Metabolite	Inflammation/Immunology Neurological Disease
Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.

HY-135654

hDHODH-IN-2	Lactate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
hDHODH-IN-2 is an analogue of the active metabolite of Leflunomide. hDHODH-IN-2 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory activity.

HY-W050000

OR-1855	Potassium Channel Phosphodiesterase (PDE) Autophagy	Cardiovascular Disease
OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.

HY-135827

MSC2360844	PI3K	Cancer Inflammation/Immunology
MSC2360844 is a potent, orally active and selective *PI3Kδ* inhibitor, with an IC₅₀ of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.

HY-130233

S516	Microtubule/Tubulin	Cancer
S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC₅₀ of 4.29 μM. S516 has marked antitumor activity.

HY-18341A

L-Thyroxine sodium salt pentahydrate Sodium levothyroxine pentahydrate	Thyroid Hormone Receptor	Endocrinology
L-Thyroxine sodium salt pentahydrate (Levothyroxine; T4) is a synthetic hormone in the treatment of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).

HY-16031

AFP464 free base NSC710464 free base	HIF/HIF Prolyl-Hydroxylase	Cancer
AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC₅₀ of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.

HY-14949

Cevipabulin TTI-237	Microtubule/Tubulin	Cancer
Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [³H] vinblastine to tubulin, with an IC₅₀ of 18-40 nM for cytotoxicity in human tumor cell line.

HY-100528

Nanchangmycin Nanchangmycin A	Bacterial Antibiotic	Infection
Nanchangmycin, a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.

HY-N2543

Damascenone (E/Z)-Damascenone	NF-κB	Inflammation/Immunology
Damascenone ((E/Z)-Damascenone) is an active compound of Epipremnum pinnatum with anti-inflammatory activity. Damascenone is a mixture complex of E-isomer-Damascenone and Z-isomer Damascenone.

HY-17388

(±)-Huperzine A	AChE	Neurological Disease
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

HY-N1455

Falcarinol Panaxynol; Carotatoxin	HSP	Cancer
Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.

HY-14532

Brincidofovir CMX001; HDP-CDV	CMV	Infection
Brincidofovir (CMX001; HDP-CDV) is an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.

HY-B1130

Isoxicam	COX	Inflammation/Immunology
Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis. Isoxicam is a nonselective inhibitor of COX-1 and *COX-2*.

HY-112542

Nemadectin CL-287088; LL-F28249 α	Parasite Antibiotic	Infection
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.

HY-11070

MK-0952	Phosphodiesterase (PDE)	Neurological Disease
MK-0952 is a selective and orally active PDE4 inhibitor, with an IC₅₀ of 0.53 nM. MK-0952 has the potential for Alzheimer’s disease study.

HY-135380

Atorvastatin acetonide tert-butyl ester	Others	Cardiovascular Disease
Atorvastatin acetonide tert-butyl ester is a useful pharmaceutical intermediate in the preparation of Atorvastatin salts. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

HY-P0184A

Camstatin TFA	NO Synthase	Neurological Disease
Camstatin TFA, a functionally active 25-residue fragment of PEP-19's IQ motif, binds calmodulin and inhibits neuronal nitric oxide (NO) synthase.

HY-10003

Alfacalcidol 1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3	VD/VDR	Metabolic Disease
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.

HY-10231

PX-478
HIF/HIF Prolyl-Hydroxylase Autophagy Cancer

PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.

HY-12883A

PF-05198007	Sodium Channel	Neurological Disease
PF-05198007 is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.

HY-32219

T863	Acyltransferase	Metabolic Disease
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.

HY-16278

Pradigastat LCQ-908	Acyltransferase	Metabolic Disease
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

HY-N1376

20(R)-Ginsenoside Rg3 20(R)-Propanaxadiol; R-ginsenoside Rg3	Others	Cancer
20(R)-ginsenoside Rg3 (20(R)-Propanaxadiol), one of the active compounds present in ginseng root, has a potent angiosuppressive and antitumor activities.

HY-10213A

SNX-5422 Mesylate PF-04929113 (Mesylate)	HSP	Cancer
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a K_d of 41 nM, and also induces Her-2 degradation, with an IC₅₀ of 37 nM.

HY-B1263

Chlorobutanol	Bacterial Fungal	Infection Neurological Disease
Chlorobutanol is a pharmaceutical preservative with sedative-hypnotic actions. Chlorobutanol is active against a wide variety of Gram-positive and Gram-negative bacteria, and several mold spores and *fungi*.

HY-106147B

Frakefamide TFA	Opioid Receptor	Neurological Disease
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

HY-N2058

Neogambogic acid	Bacterial Apoptosis	Cancer Infection
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA).

HY-115499

MPC-0767
HSP Cancer

MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability.

HY-108619

Gisadenafil besylate UK 369003-26	Phosphodiesterase (PDE)	Neurological Disease
Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

HY-W010144

Phenidone	COX Lipoxygenase	Inflammation/Immunology Cardiovascular Disease
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat.

HY-101125A

L-45 dihydrochloride L-Moses dihydrochloride	Epigenetic Reader Domain	Cancer
L-45 dihydrochloride (L-Moses dihydrochloride) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a K_d of 126±15 nM.

HY-14185

Lixivaptan VPA-985; WAY-VPA 985	Vasopressin Receptor	Cardiovascular Disease Endocrinology
Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC₅₀ values of 1.2 and 2.3 nM for human and rat V2, respectively.

HY-112441

Prolyl Hydroxylase inhibitor 1	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC₅₀ of 62.23 nM. Antianemia agent.

HY-131338

RORγt inverse agonist 13	ROR	Inflammation/Immunology
RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC₅₀ of 63.8 nM.

HY-120508

Pivanex AN-9; Pivalyloxymethyl butyrate	HDAC Bcr-Abl Apoptosis	Cancer Inflammation/Immunology
Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.

HY-114436

MRTX-1257
Ras Cancer

MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.

HY-11087

SD 0006 SD-06	p38 MAPK Autophagy	Inflammation/Immunology
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC₅₀ of 110 nM for p38α.

HY-18632A

GSK2879552 dihydrochloride	Histone Demethylase	Cancer
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

HY-112314

AZD0424	Src Bcr-Abl Apoptosis	Cancer
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.

HY-17387

(-)-Huperzine A Huperzine A	AChE Apoptosis	Neurological Disease
(-)-Huperzine A (Huperzine A), an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

HY-10527C

Telatinib mesylate Bay 57-9352 mesylate	VEGFR PDGFR c-Kit	Cancer
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active *VEGFR2, VEGFR3, PDGFα, and c-Kit* inhibitor with IC₅₀s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

HY-10167A

Tecalcet Hydrochloride R-568 (hydrochloride)	CaSR	Others
Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca²⁺.

HY-N0602

Ginsenoside Rg2 Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2	NF-κB Amyloid-β	Neurological Disease Cardiovascular Disease Cancer
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces Aβ_1-42 accumulation.

HY-W067479

(E)-Cinnamamide	Others	Others
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effectiveness as a non-lethal chemical repellent suitable for reducing avian pest damage.

HY-N0738

Stachydrine hydrochloride	NF-κB	Cardiovascular Disease Cancer
Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.

HY-N1481

Methyl linoleate	Others	Metabolic Disease
Methyl linoleate, a major active constituent of Sageretia thea fruit (HFSF), is a major anti-melanogenic compound. Methyl linoleate downregulates microphthalmia-associated transcription factor (MITF) and tyrosinase-related proteins.

HY-13463

Avatrombopag E5501; AKR-501; YM477	Thrombopoietin Receptor	Inflammation/Immunology
Avatrombopag (E5501; AKR-501; YM477) is an orally-active thrombopoietin (TPO) receptor agonist with an EC₅₀ value of 3.3 nM and may be useful in the treatment of patients with thrombocytopenia.

HY-10309

Sibrafiban RO 48-3657	Integrin	Cardiovascular Disease
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.

HY-135653

EC5026 BPN-19186	Epoxide Hydrolase	Neurological Disease
EC5026 (BPN-19186) is a first-in-class, non-opioid and orally active soluble Epoxide Hydrolase (sEH) inhibitor. EC5026 shows efficacy for inflammatory and neuropathic pain.

HY-120142

EC359	Apoptosis	Cancer
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.

HY-108017

Ferric maltol	Others	Metabolic Disease
Ferric maltol is an orally active complex of a single ferric ion (Fe³⁺). Ferric maltol has tha potential for iron deficiency anemia treatment in inflammatory bowel disease.

HY-B0834

Indoxacarb (±)-Indoxacarb	Sodium Channel
Indoxacarb ((±)-Indoxacarb) is a broad-spectrum oxadiazine insecticide. Indoxacarb is metabolized in vivo to its active N-decarbomethoxyllated metabolite DCJW. Indoxacarb suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons.

HY-B0955

Oxethazaine Oxetacaine	HBV	Neurological Disease
Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.

HY-B1256A

Cefuroxime	Bacterial Antibiotic	Infection
Cefuroxime is an orally active second-generation cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime has a broad spectrum activity against Gram-positive and Gram-negative bacteria.

HY-101215

Evobrutinib M2951; MSC2364447C	Btk	Inflammation/Immunology Cancer
Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC₅₀ of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases.

HY-136447

ASP4132	AMPK	Cancer
ASP4132 is an orally active, potent AMPK activator with an EC₅₀ of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.

HY-B1691

Methenamine hippurate Hexamine hippurate	Bacterial	Cancer
Methenamine hippurate (Hexamine hippurate) is an orally active urinary antiseptic agent with a wide antibacterial spectrum. Methenamine hippurate is effective against most common urinary tract pathogens.

HY-126290

Tyk2-IN-8	JAK	Inflammation/Immunology
Tyk2-IN-8 (compound 10) is a selective *TYK2* inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC₅₀ of 17 nM, used in the treatment of psoriasis.

HY-118828

12-Oxo phytodienoic acid 12-OPDA	Bacterial
12-Oxo phytodienoic acid is a biologically active, immediate precursor of 7-epi jasmonic acid. 12-Oxo phytodienoic acid appears to play an independent role in mediating resistance to pathogens and pests.

HY-10396

Emricasan PF 03491390; IDN-6556	Caspase Influenza Virus	Cancer Infection Neurological Disease
Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in *caspase-3* activity and protected human cortical neural progenitors.

HY-13275

IRAK inhibitor 1	IRAK	Inflammation/Immunology
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC₅₀ of 216 nM, is poorly active against JNK-1 and JNK-2 with IC₅₀ of 3.801 μM, and >10 μM, respectively.

HY-135648

PfDHODH-IN-1	Parasite Lactate Dehydrogenase DNA/RNA Synthesis	Infection
PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity.

HY-136703

Lopinavir Metabolite M-1	HIV Protease	Infection
Lopinavir Metabolite M-1 is an active metabolite of Lopinavir, and inhibits HIV protease with a K_i of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro.

HY-108908

(Rac)-Modipafant UK-74505	Others	Infection Inflammation/Immunology
(Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection.

HY-135392

N-Desmethyl Pimavanserin AC-279	Drug Metabolite
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-18343A

CP-31398 dihydrochloride
MDM-2/p53 Cancer

CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.

HY-15439

(24S)-24,25-Dihydroxyvitamin D3 (24S)-24,25-Dihydroxycholecalciferol	VD/VDR	Others
(24S)-24,25-Dihydroxycholecalciferol is an inactive form of vitamin D3 which undergoes various levels of hydroxylation to form active vitamin D3 analogs.

HY-101979

CB-1158 INCB01158	Arginase	Cancer
CB-1158 (INCB01158) is a potent and orally active inhibitor of arginase, with IC₅₀s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent.

HY-N0495

Aloenin Aloenin A	Beta-secretase	Neurological Disease
Aloenin (Aloenin A) is a class of anthraquinones isolated from Aloe arborescens. Aloenin has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).

HY-135847

Desmethyl ferroquine SSR97213	Parasite Drug Metabolite	Infection
Desmethyl ferroquine (SSR97213) is the active and major metabolite of Ferroquine. Ferroquine is an antimalarial. Desmethyl ferroquine shows significant activity against Chloroquine-susceptible and resistant P. falciparum strains.

HY-17643

Oteseconazole VT-1161	Fungal Cytochrome P450	Infection
Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (K_d, <39 nM), shows no obvious effect on human CYP51.

HY-123291

SM-276001	Toll-like Receptor (TLR) IFNAR	Cancer Inflammation/Immunology
SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.

HY-135379

Atorvastatin acetonide	Others	Cardiovascular Disease
Atorvastatin acetonide is an impurity of Atorvastatin, and extracted from patent WO2011131605A1, Compound 4. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

HY-120635

BMS-1001 hydrochloride	PD-1/PD-L1	Cancer Inflammation/Immunology
BMS-1001 hydrochloride is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 hydrochloride exhibits low-toxicity in cells.

HY-136255

AZD-9833
Estrogen Receptor/ERR Cancer

AZD-9833 is a potent and orally active estrogen receptor (ER) antagonist. AZD-9833 is used for the study of ER⁺ HER2-advanced breast cancer.

HY-135270

ADRA1D receptor agonist 1	Adrenergic Receptor	Endocrinology
ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α_1D adrenoceptor antagonist, with a K_i of 1.6 nM.

HY-B1256

Cefuroxime sodium	Bacterial Antibiotic	Infection
Cefuroxime sodium is an orally active second-generation cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime sodium has a broad spectrum activity against Gram-positive and Gram-negative bacteria.

HY-101979A

CB-1158 dihydrochloride INCB01158 dihydrochloride	Arginase	Cancer
CB-1158 dihydrochloride (INCB01158 dihydrochloride) is a potent and orally active inhibitor of arginase, with IC₅₀s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent.

HY-N1362

Salvianolic acid B Lithospermic acid B	Autophagy	Cardiovascular Disease
Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.

HY-U00112

Estradiol 3-sulfamate BLE 00084; E2MATE; ES-J 995	Others	Cancer
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC₅₀ of 251 nM and a K_i of 133 nM.

HY-112726

PXS-4728A	Monoamine Oxidase	Inflammation/Immunology
PXS-4728A is a selective, orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO). PXS-4728A ameliorates chronic obstructive pulmonary disease in mice.

HY-131312

Mutant IDH1-IN-6	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.

HY-B0592S

Trandolapril D5 RU44570 D5	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Trandolapril D5 (RU44570 D5) is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF).

HY-B1106

Tetrahydroxyquinone Tetrahydroxy-1,4-benzoquinone; Tetrahydroxybenzoquinone	Reactive Oxygen Species	Cancer
Tetrahydroxyquinone is a molecule best known as a primitive anticataract drug, is also a highly redox active molecule that can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS).

HY-100888

Simurosertib TAK-931	CDK	Cancer
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC₅₀ of <0.3 nM. Simurosertib has anti-cancer activity.

HY-12885C

ADU-S100 enantiomer ammonium salt MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt	Others	Inflammation/Immunology
ADU-S100 enantiomer ammonium salt (MIW815 enantiomer ammonium salt) is the less active enantiomer of ADU-S100. ADU-S100 is an activator of stimulator of interferon genes (STING).

HY-107051

GW 766994 GW 994	CCR	Inflammation/Immunology Endocrinology
GW 766994 (GW 994) is an orally active and specific chemokine receptor-3 (CCR3) antagonist. GW 766994 has the potential for asthma and eosinophilic bronchitis research.

HY-101472

Closthioamide	Bacterial	Infection
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.

HY-15005A

PSI-7976	HCV	Infection
PSI-7976 is the isomer of PSI-7977. PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-16780

Gemilukast ONO-6950	Leukotriene Receptor	Inflammation/Immunology
Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT₁ and CysLT₂) antagonist, with IC₅₀s of 1.7, 25 nM for human CysLT₁ and CysLT₂, respectively.

HY-105124A

Bufuralol hydrochloride Ro 3-4787 hydrochloride	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.

HY-109040

Quilseconazole VT-1129	Fungal Cytochrome P450	Infection
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.

HY-101516

CYP17-IN-1
Cytochrome P450 Cancer

CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC₅₀s of 15.8 and 20.1 nM.

HY-133013

GLPG-3221	CFTR	Inflammation/Immunology
GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC₅₀ of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.

HY-135910

3,4-Dehydro Cilostazol OPC-13015	Drug Metabolite	Cancer Cardiovascular Disease
3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study.

HY-10617

Rucaparib phosphate AG-014699 phosphate; PF-01367338 phosphate	PARP	Cancer
Rucaparib phosphate (AG-014699 phosphate) is an orally active and potent PARP inhibitor, with a K_i of 1.4 nM for PARP1 in cell-free assay. Rucaparib phosphate shows binding affinity to eight other PARP domains.

HY-135815

Mobocertinib TAK-788; AP32788	EGFR	Cancer
Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and *HER2* oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.

HY-136560

6-Azathymine acid	Drug Metabolite	Others
6-Azathymine acid is a metabolite of Pymetrozine. Pymetrozine is active against plant-sucking insects, such as aphids and whiteflies in vegetables, cotton, field crops and fruits and affects the nervous regulation of feeding behavior.

HY-136439

4-Epianhydrotetracycline hydrochloride	Bacterial Antibiotic
4-Epianhydrotetracycline hydrochloride is a degradation product of the antibiotic tetracycline. 4-Epianhydrotetracycline hydrochloride is active against *Pseudomonas, Agrobacterium, Moraxella, Bacillus, and E. coli* (MIC₅₀s = 0.75-16 mg/L).

HY-14200

(S)-Rasagiline TVP1022; S-PAI	Monoamine Oxidase	Neurological Disease
(S)-Rasagiline (TVP1022) is the S-isomer of Rasagiline, which is an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor.

HY-129239

ASLAN003	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
ASLAN003 is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) which has the potential to be a first-in-class candidate in AML (Acute Myelogenous Leukemia). ASLAN003 has antitumor activity.

HY-10617A

Rucaparib AG014699; PF-01367338	PARP	Cancer
Rucaparib (AG014699) is an orally active and potent inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay. Rucaparib shows binding affinity to eight other PARP domains.

HY-N2877

Annonacin	Potassium Channel Sodium Channel Na+/K+ ATPase Calcium Channel	Neurological Disease
Annonacin is an Acetogenin and promotes cytotoxicity via a pathway inhibiting the mitochondrial complex. Annonacin is the active agent found in Graviola leaf extract to act as an inhibitor of sodium/potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps.

HY-135407S

N-Desethyl Oxybutynin D5 hydrochloride	Drug Metabolite	Neurological Disease
N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K⁺ channels.

HY-12837

EN460	Others	Others
EN460 is a small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1); interacts selectively(IC50=1.9 uM) with the reduced, active form of ERO1α and prevents its reoxidation.

HY-101731

CP-96021 hydrochloride	Leukotriene Receptor	Inflammation/Immunology
CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with K_i values of 34 nM and 37 nM, respectively.

HY-108036

Pro-xylane Hydroxypropyl tetrahydropyrantriol	Others	Metabolic Disease
Pro-xylane (Hydroxypropyl tetrahydropyrantriol) is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis. Pro-xylane is the first example of 'Green' chemical used in cosmetic.

HY-B1301

Triprolidine hydrochloride monohydrate	Histamine Receptor	Neurological Disease
Triprolidine hydrochloride monohydrate is an orally active, cell-permeable and first-generation histamine H1 antagonist. Triprolidine hydrochloride monohydrate is an antihistamine and can be used in allergic rhinitis; asthma; and urticaria.

HY-14200A

(S)-Rasagiline mesylate TVP1022 (mesylate); S-PAI mesylate	Monoamine Oxidase	Neurological Disease
(S)-Rasagiline (TVP1022) mesylate is the S-isomer of rasagiline, which is an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor.

HY-106723

AMP-PCP
HSP Cancer

AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a K_d value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90.

HY-101671

S-methyl-KE-298 M-2	MMP Drug Metabolite	Inflammation/Immunology
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.

HY-19498

WAY-204688 SIM-688	NF-κB	Inflammation/Immunology
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC₅₀ of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

HY-101653

MHP 133	AChE mAChR 5-HT Receptor	Neurological Disease
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with K_i of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

HY-14305A

BMS-582949 hydrochloride	p38 MAPK Autophagy	Inflammation/Immunology
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC₅₀ of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.

HY-135827A

MSC2360844 hemifumarate	PI3K	Cancer Inflammation/Immunology
MSC2360844 hemifumarate is a potent, orally active and selective *PI3Kδ* inhibitor, with an IC₅₀ of 145 nM. MSC2360844 hemifumarate shows highly selective against a panel of 278 additional kinases.

HY-14949C

Cevipabulin fumarate TTI-237 fumarate	Microtubule/Tubulin	Cancer
Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [³H]NSC 49842 to tubulin, with an IC₅₀ of 18-40 nM for cytotoxicity in human tumor cell line.

HY-N1995

Methylswertianin	Others	Metabolic Disease
Methylswertianin is an active constituent in Swertia punicea Hemsl, with anti-diabetic effect. Methylswertianin could be useful for treating type-2 diabetes, likely via the improvement of insulin resistance (IR).

HY-100528A

Dianemycin Nanchangmycin free acid	Bacterial Antibiotic	Infection
Dianemycin (Nanchangmycin free acid), a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.

HY-136589

Verapamil EP Impurity C hydrochloride NSC-609249 hydrochloride	Calcium Channel P-glycoprotein Cytochrome P450	Metabolic Disease
NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

HY-N3961

Neoglycyrol	Others	Cardiovascular Disease
Neoglycyrol is isolated from the root of Glycyrrhiza uralensis Fisch. Neoglycyrol is a potential myocardial protection active compound screened from traditional patent medicine Tongmai Yangxin pill (TMYXP).

HY-107410

SC-26196	Others	Inflammation/Immunology
SC-26196 is a potent, orally active Delta6 desaturase (D6D) inhibitor (IC₅₀=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties.

HY-115292

Simvastatin sodium	HMG-CoA Reductase (HMGCR)	Cancer
Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a K_i value of 0.12 nM.

HY-104075

R916562	TAM Receptor VEGFR	Cancer
R916562 is an orally active and selective *Axl/VEGF-R2* inhibitor with IC₅₀s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.

HY-19908B

(R)-BAY-85-8501	Others	Metabolic Disease
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC₅₀ of 65 pM.

HY-131181

LEI-401	Phospholipase	Neurological Disease
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC₅₀ of 27 nM. LEI-401 modulates emotional behavior in mice.

HY-15005S1

Sofosbuvir D6 PSI-7977 D6; GS-7977 D6	HCV	Others
Sofosbuvir D6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-15084A

(-)-Dizocilpine maleate (-)-MK-801 maleate	iGluR	Neurological Disease
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a K_i of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.

HY-19522A

Seladelpar sodium salt MBX-8025 sodium salt; RWJ-800025 sodium salt	PPAR	Metabolic Disease
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC₅₀ of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

HY-N6607

Tryptanthrin	Others	Inflammation/Immunology
Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin inhibits LT formation in human whole blood (IC₅₀ = 10 µM) and reduces LTB4 levels in the rat pleurisy model.

HY-14293

NVP-DPP728 dihydrochloride	Dipeptidyl Peptidase	Metabolic Disease
NVP-DPP728 dihydrochloride is a potent, selective and orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with a K_i of 11 nM. NVP-DPP728 dihydrochloride can be used for the research of diabetes mellitus.

HY-N7560

Safranal	Others	Inflammation/Immunology Neurological Disease
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.

HY-10999

Trametinib GSK1120212; JTP-74057	MEK Autophagy Apoptosis	Cancer
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC₅₀s of about 2 nM. Trametinib activates autophagy and induces *apoptosis*.

HY-100310

N-type calcium channel blocker-1	Calcium Channel	Neurological Disease
N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC₅₀ of 0.7 μM in the IMR32 assay.

HY-117288A

S55746 hydrochloride BLC201 (hydrochloride)	Bcl-2 Family	Cancer
S55746 hydrochloride (BLC201 hydrochloride) is a potent, orally active and selective *BCL-2* inhibitor, with a K_i of 1.3 nM and a K_d of 3.9 nM. S55746 hydrochloride (BLC201 hydrochloride) has antitumor activity with low toxicity.

HY-17600S

Acalabrutinib D4 ACP-196 D4	Btk	Cancer
Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.

HY-114384

NV-5138	mTOR	Neurological Disease
NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 possesses rapid antidepressant effects.

HY-130353

Desethylamiodarone hydrochloride N-desethylamiodarone hydrochloride; LB 33020 hydrochloride	Potassium Channel Autophagy	Cardiovascular Disease
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

HY-108908A

Modipafant UK-80067	Others	Inflammation/Immunology
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.

HY-13784

Pirodavir R77975	Enterovirus	Infection
Pirodavir is a potent, broad-spectrum picornavirus inhibitor, and is highly active against both group A and group B rhinovirus serotypes. Pirodavir is very potent in a virus yield reduction assay (IC₉₀=2.3 nM).

HY-128606

Thiamine diphosphate analog 1	Others	Metabolic Disease
Thiamine diphosphate analog 1 is an analog of Thiamine diphosphate. Thiamine diphosphate is the active form of vitamin B₁. Thiamine diphosphate a universal cofactor involved in pivotal cellular pathways.

HY-108012

ME1111	Fungal	Infection
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research.

HY-N2382

Polyphyllin H	Others	Inflammation/Immunology Neurological Disease
Polyphyllin H, the major active component isolated from Rhizoma Paridis (named chonglou in Chinese), have been widely used in traditional Chinese medicinal preparations to treat inflammation, fracture and convulsion.

HY-12459

Pyrindamycin B	Bacterial	Infection
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice.

HY-135398

Decarboxy Moxifloxacin	Others	Inflammation/Immunology Infection
Decarboxy Moxifloxacin (compound 8) is a decarboxylated compound of Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.

HY-135387

4-Desmethyl Istradefylline	Drug Metabolite	Neurological Disease
4-Desmethyl Istradefylline is a metabolite of Istradefylline. 4-Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with K_i of 2.2 nM in experimental models of Parkinson's disease.

HY-13569A

Beraprost sodium	Prostaglandin Receptor	Inflammation/Immunology Cardiovascular Disease
Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of *PGI2. Beraprost sodium is a potent vasodilator*, has the potential for pulmonary arterial hypertension treatment through expanding renal vessels, improving microcirculation.

HY-135655A

SPR720
pVXc-486
Bacterial Infection

SPR720 (pVXc-486) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). SPR720 has potent bactericidal activities in vivo.

HY-117880

Exicorilant CORT 125281	Glucocorticoid Receptor	Metabolic Disease Endocrinology
Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a K_i value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia.

HY-120085

PFE-360 PF-06685360	LRRK2	Neurological Disease
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC₅₀ of 2.3 nM in vivo.

HY-N2905

Aurantiamide acetate Asperglaucide	Cathepsin	Inflammation/Immunology
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases.

HY-10133

β-Secretase Inhibitor IV	Beta-secretase	Neurological Disease
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC₅₀s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

HY-N0478

Neoline Bullatine B	Others	Neurological Disease
Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain.

HY-109019

Vorolanib CM082; X-82	VEGFR PDGFR	Cancer
Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor. Vorolanib minimizes toxicity, disrupts tumor angiogenesis and tumor cell proliferation, and induces of tumor cell death.

HY-12352A

HJC0416 hydrochloride	STAT Apoptosis	Cancer
HJC0416 hydrochloride is a potent and orally active *STAT3* inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.

HY-13943

CNX-774	Btk	Cancer
CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.

HY-N0268

Irisflorentin	NO Synthase	Inflammation/Immunology
Irisflorentin, a naturally occurring isoflavone, is an abundant active constituent in Rhizoma Belamcandae. Irisflorentin markedly reduces the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. Anti-inflammatory activity.

HY-B0977

Dicloxacillin Sodium hydrate Dicloxacillin sodium salt monohydrate	Bacterial Antibiotic	Infection
Dicloxacillin Sodium hydrate (Dicloxacillin sodium salt monohydrate) is a narrow-spectrum β-Lactam antibiotic of the penicillin class, is used to treat infections caused by susceptible Gram-positive bacteria, active against beta-lactamase-producing organisms such as Staphylococcus aureus.

HY-118047

CI 972 anhydrous	Nucleoside Antimetabolite/Analog	Inflammation/Immunology
CI 972 anhydrous is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (K_i=0.83 μM) under development as a T cell-selective immunosuppressive agent.

HY-117071

Dabuzalgron Ro 115-1240	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.

HY-106541

Neticonazole	Fungal	Cancer Infection
Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole has anti-infection and anti-cancer effects.

HY-13848

AZD8797	CXCR	Inflammation/Immunology Endocrinology
AZD8797 is an allosteric non-competitive and orally active antagonist of the human *CX3CR1* receptor; antagonizes CX3CR1 and CXCR2 with K_is of 3.9 and 2800 nM, respectively.

HY-10392

Sutezolid PNU-100480; U-100480; PF-02341272	Bacterial Antibiotic	Infection
Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis.

HY-14184

Macitentan ACT-064992	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

HY-15005S

Sofosbuvir 13CD3 PSI-7977 13CD3; GS-7977 13CD3	HCV	Infection
Sofosbuvir 13CD3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

HY-B1500

2,2,2-Trichloroethanol	Potassium Channel	Neurological Disease
2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K_2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

HY-131256

Cetirizine Impurity C	Histamine Receptor	Endocrinology Inflammation/Immunology
Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist^{[1]^{^{[2] .}}}

HY-13318

Oseltamivir acid GS 4071; Ro 64-0802; Oseltamivir carboxylate	Influenza Virus Drug Metabolite	Infection
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of *influenza virus neuraminidase (IC₅₀=2* nM)** with activity against both influenza A and B viruses.

HY-B1730

Phensuximide	Others	Metabolic Disease Neurological Disease
Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.

HY-136185

Atorvastatin Epoxy Tetrahydrofuran Impurity	Others	Others
Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.

HY-107798

Potassium guaiacolsulfonate hemihydrate	Bacterial	Infection
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs.

HY-N4288

4-Methylesculetin	Glutathione Peroxidase	Inflammation/Immunology Cancer
4-Methylesculetin is an orally active natural coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity and reduces IL-6 level.

HY-117288

S55746 BLC201	Bcl-2 Family	Cancer
S55746 (BLC201) is a potent, orally active and selective *BCL-2* inhibitor, with a K_i of 1.3 nM and a K_d of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity.

HY-135868

Mito-apocynin (C2)	Mitochondrial Metabolism	Neurological Disease
Mito-apocynin (C2), an orally active mitochondria-targeted triphenylphosphonium (TPP)-based compound, is synthesized by conjugating the Apocynin moiety with a TPP ⁺ cation. Mito-apocynin (C2) exhibits antineuroinflammatory effect.

HY-13738A

Raloxifene hydrochloride Keoxifene hydrochloride; LY156758; LY139481 hydrochloride	Estrogen Receptor/ERR Autophagy	Endocrinology Cancer
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

HY-122907

JNJ4796	Influenza Virus	Infection
JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs).

HY-128365

Neticonazole hydrochloride	Fungal	Cancer Infection
Neticonazole hydrochloride is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole hydrochloride is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole hydrochloride has anti-infection and anti-cancer effects.

HY-111617

BTR-1
Apoptosis Cancer

BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.

HY-133141

DI-87	Others	Cancer
DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC₅₀ of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.

HY-19336

BAZ2-ICR	Epigenetic Reader Domain	Cancer
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC₅₀s of 130 nM and 180 nM, and K_ds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding *BAZ2A/B* over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.

HY-12628

GNE-618	Nampt	Cancer
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC₅₀ of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.

HY-N0929

Hexahydrocurcumin	COX Reactive Oxygen Species	Cancer
Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active *COX-2* inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities.

HY-100888A

(R)-Simurosertib (R)-TAK-931	Others	Others
(R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC₅₀ of <0.3 nM .

HY-B1526

Thiacetazone Thioacetazone; Amithiozone	Bacterial	Infection
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of *Mycobacterium tuberculosis H37Rv* with a MIC value of 0.1 μg/mL.

HY-125506

NP-G2-044
Others Cancer

NP-G2-044 is a potent, orally active fascin inhibitor, with an IC₅₀ of ~2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response.

HY-108256

Melitracen hydrochloride	5-HT Receptor	Neurological Disease
Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.

HY-17358

Loteprednol Etabonate	Glucocorticoid Receptor Bacterial Antibiotic	Infection Endocrinology Inflammation/Immunology
Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology.

HY-N7068

Mupirocin calcium hydrate	Bacterial Antibiotic	Infection Inflammation/Immunology
Mupirocin calcium hydrate is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.

HY-103040

Zuranolone	GABA Receptor	Neurological Disease
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABA_A receptor, with EC₅₀s of 296 and 163 nM for *α₁β₂γ₂* and α₄β₃δ GABA_A receptors, respectively.

HY-109137

Selgantolimod GS-9688	Toll-like Receptor (TLR) HBV	Infection
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.

HY-W002484

3-Hydroxy-4-methoxyacetophenone Acetoisovanillone; Isoacetovanillone	Others	Inflammation/Immunology
3-Hydroxy-4-methoxyacetophenone(Acetoisovanillone; Isoacetovanillone) is an active compound isolated from P. spinosa. Isoacetovanillone possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon.

HY-106723A

AMP-PCP disodium	HSP	Cancer
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a K_d value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90.

HY-19447

Besifovir LB80331	HBV	Infection
Besifovir (LB80331), a parent drug converted by LB80380, further metabolizes to its active form, LB80317. LB80380 is potent antiviral agent against hepatitis B virus (HBV) ^[1].

HY-N2460

Aloesin Aloeresin	Others	Cancer Inflammation/Immunology
Aloesin (Aloeresin) is an active constituent of the herb aloe vera and displays anti-inflammatory activity, ultraviolet protection, and antibacterium effects. Aloesin exerts its anticancer effect through the MAPK signaling pathway.

HY-15761

AZD2858	GSK-3	Neurological Disease
AZD2858 is a potent, orally active *GSK-3* inhibitor, with IC₅₀s of 0.9 and 5 nM for *GSK-3α* and *GSK-3β*, respectively, used in the research of fracture healing.

HY-101549

MRX-2843 UNC2371	FLT3	Cancer
MRX-2843 (UNC2371) is an orally active dual MERTK and *FLT3* tyrosine kinases inhibitor (TKI) with enzymatic IC₅₀s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.

HY-136610

Chlorpyrifos-oxon	AChE	Neurological Disease
Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.

HY-B2158

Chlorotrianisene	Estrogen Receptor/ERR COX	Endocrinology Cardiovascular Disease
Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.

HY-101140A

KI696 isomer	Keap1-Nrf2	Metabolic Disease Inflammation/Immunology
KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.

HY-135914

JBJ-02-112-05
EGFR Cancer

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 15 nM for EGFR^L858R/T790M.

HY-P1495

Small Cardioactive Peptide B SCPB	Adenylate Cyclase	Neurological Disease Cardiovascular Disease
Small Cardioactive Peptide B (SCP_B), a neurally active peptide, stimulates adenylate cyclase activity in particulate fractions of both heart and gill tissues with EC₅₀s of 0.1 and 1.0 μM, respectively.

HY-135375

O-Methyl Atorvastatin hemicalcium	Others	Metabolic Disease Inflammation/Immunology
O-Methyl Atorvastatin (hemicalcium) is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids.

HY-135815A

Mobocertinib succinate TAK-788 succinate; AP32788 succinate	EGFR	Cancer
Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and *HER2* oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.

HY-101564

JNJ-64619178	Histone Methyltransferase	Cancer
JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.

HY-133122

UCB-9260	TNF Receptor	Inflammation/Immunology
UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar K_d of 13 nM.

HY-108036A

(S)-Pro-xylane (S)-Hydroxypropyl tetrahydropyrantriol	Others	Others
(S)-Pro-xylane ((S)-Hydroxypropyl tetrahydropyrantriol) is the S-enantiomer of Pro-xylane (HY-108036). Pro-xylane is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis.

HY-135373

Desfluoro-atorvastatin	Others	Metabolic Disease Inflammation/Immunology
Desfluoro-atorvastatin is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids.

HY-N6826

Asatone	NF-κB	Inflammation/Immunology
Asatone is an active component isolated from Radix et Rhizoma Asari, with anti-inflammatory effect via activation of NF-κB and donwn regulation of p-MAPK (ERK, JNK and p38) pathways.

HY-128337

AN7973	Parasite	Infection
AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting drug candidate for treating cryptosporidiosis.

HY-13704

SN-38 NK012	Topoisomerase ADC Cytotoxin Autophagy	Cancer
SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC₅₀s of 0.077 and 1.3 μM, respectively.

HY-106579

Tiaprofenic acid	COX	Inflammation/Immunology
Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.

HY-110201

Estrogen receptor modulator 1	Estrogen Receptor/ERR	Cancer
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC₅₀ of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.

HY-100330

YM348
5-HT Receptor Metabolic Disease

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

HY-18172

KCC2 blocker 1	Potassium Channel	Neurological Disease
KCC2 blocker 1 is an orally active and selective K⁺-Cl^- cotransporter *KCC2* blocker with an IC₅₀ of 1 μM. KCC2 blocker 1 is a benzyl prolinate and has antiepileptic effect.

HY-100405

FTIDC	mGluR	Neurological Disease
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC₅₀ of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.

HY-10959

RG7112 RO5045337	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed *MDM2-p53* inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2.

HY-17013A

Dofequidar fumarate MS-209	P-glycoprotein	Cancer
Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.

HY-112215

ARQ 531	Btk	Cancer Inflammation/Immunology
ARQ 531 is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC₅₀s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

HY-N0045

Ginsenoside Rg1 Panaxoside A; Panaxoside Rg1	Amyloid-β NF-κB Apoptosis	Inflammation/Immunology Neurological Disease Cancer
Ginsenoside Rg1 is one of the major active components of ginseng. Ginsenoside Rg1 displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

HY-13696

MSX-122	CXCR	Cancer Inflammation/Immunology Endocrinology
MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC₅₀ of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.

HY-14184A

Macitentan (n-butyl analogue)	Endothelin Receptor	Cardiovascular Disease Endocrinology
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

HY-106235

LB80317	HBV DNA/RNA Synthesis	Infection
LB80317 is an active metabolite of LB80380 and suppresses the DNA synthesis of HBV with an EC₅₀ of 0.5 μM. LB80317 has antiviral effect and has the potential for chronic hepatitis B treatment.

HY-114409

GB1107	Galectin	Cancer
GB1107 is a potent, selective, orally active inhibitor of **Galectin-3 (Gal-3) with a K_d** of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.

HY-120012

AZD9567	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC₅₀ of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.

HY-112707

AM9405	Cannabinoid Receptor 5-HT Receptor	Neurological Disease
AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC₅₀s of 45.71 and 0.076 nM, respectively.

HY-N5024

Gambogenic acid	Histone Methyltransferase	Cancer
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of *EZH2, specifically and covalently binds to Cys668 within the EZH2-SET* domain, and induces EZH2 ubiquitination.

HY-111752

EML4-ALK kinase inhibitor 1	ALK	Cancer
EML4-ALK kinase inhibitor 1 is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC₅₀ of 1 nM.

HY-N0769

Isopimpinellin	DNA/RNA Synthesis Parasite	Cancer Infection Inflammation/Immunology
Isopimpinellin, an orally active compound isolated from the roots of Pimpinella saxifrage. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect.

HY-100064

O-Desmethyl gefitinib	EGFR	Cancer
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC₅₀ of 36 nM in subcellular assays.

HY-N1374

Magnolin	ERK	Inflammation/Immunology
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and *ERK2* with IC₅₀s of 87 nM and 16.5 nM, respectively.

HY-100301

FR167344 free base	Bradykinin Receptor	Inflammation/Immunology Endocrinology
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC₅₀ value of 65 nM and no binding affinity for the B1 receptor.

HY-114412A

TD-0212 TFA	Angiotensin Receptor Neprilysin	Inflammation/Immunology
TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT₁) antagonist and neprilysin (NEP) inhibitor, with a pK_i of 8.9 for AT₁ and a pIC₅₀ of 9.2 for NEP.

HY-101792A

RG7800 hydrochloride RO6885247 hydrochloride	DNA/RNA Synthesis	Neurological Disease
RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC_1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.

HY-N0802

Tenuigenin Senegenin	NF-κB	Infection Inflammation/Immunology
Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect.

HY-135145

CB-103
Notch Cancer

CB-103 is a first-in-class orally active notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 has anti-tumor activity.

HY-50667

Apixaban BMS-562247-01	Factor Xa	Cardiovascular Disease
Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.

HY-111746

CWHM-1008	Parasite	Infection
CWHM-1008 is a potent and orally active antimalarial agent, with EC₅₀ values of 46 and 21 nM against drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively.

HY-N0008

Orcinol glucoside	Others	Neurological Disease
Orcinol glucoside (OG) is an active constituent isolated from Rhizoma Curculiginis, with antidepressant effects. Orcinol glucoside facilitates the shift of MSC fate to osteoblast and prevents adipogenesis via Wnt/β-catenin signaling pathway.

HY-10531

ARRY-380 (analog )	EGFR	Cancer
ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.

HY-16725

Lemborexant E-2006	Orexin Receptor (OX Receptor)	Neurological Disease
Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC₅₀ values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia.

HY-B1675

Levalbuterol (R)-Albuterol; (R)-Salbutamol; Levosalbutamol	Adrenergic Receptor	Inflammation/Immunology
Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.

HY-N2569

(-)-Curine	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
(-)-Curine is an orally active bisbenzylisoquinoline alkaloid isolated from Chondrodendron platyphyllum. (-)-Curine presents anti-inflammatory and analgesic effects at nontoxic doses, at least in part, resulting from the inhibition of prostaglandin E2 production.

HY-114379

AS2717638	LPL Receptor	Inflammation/Immunology
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC₅₀ of 38 nM for hLPA5. AS2717638 also significantly improves PGE₂-, PGF_2α-, and AMPA-induced allodynia.

HY-131343

HBV-IN-4	HBV DNA/RNA Synthesis	Infection
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC₅₀ of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.

HY-10162

Olaparib AZD2281; KU0059436	PARP Autophagy Mitophagy	Cancer
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and *PARP2, respectively. Olaparib is an autophagy* and mitophagy activator.

HY-107725

BIBO3304 TFA	Neuropeptide Y Receptor	Metabolic Disease
BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC₅₀=0.38 and 0.72 nM, respectively).

HY-Y0337A

L-Cysteine hydrochloride	Endogenous Metabolite	Metabolic Disease
L-Cysteine hydrochloride is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents and humans.

HY-B0293A

Butoconazole	Fungal	Infection
Butoconazole, an imidazole antifungal agent, is active against Candida spp. and effective against vaginal infections due to Candida albicans. Butoconazole is presumed to function as other imidazole derivatives via inhibition of steroid synthesis.

HY-16106A

(8R,9S)-Talazoparib (8R,9S)-BMN-673; (8R,9S)-LT-673	PARP	Cancer
(8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib, less active than Talazoparib on the inhibition of PARP1, with an IC₅₀ of 144 nM.

HY-N1954

Protostemonine	Others	Inflammation/Immunology
Protostemonine is an active alkaloid mainly isolated from the roots of Stemona sesslifolia, with anti-inflammatory activity. Protostemonine has anti-inflammatory effects on asthma and gram-negative bacteria-induced acute lung injury.

HY-U00193

Ro18-5362	Others	Metabolic Disease
Ro18-5362 is the less active prodrug of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H⁺+K⁺)-ATPase activity and associated proton translocation.

HY-B0352

Mirtazapine Org3770; 6-Azamianserin	5-HT Receptor	Neurological Disease
Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.

HY-135303

GLPG1205	GPR84	Inflammation/Immunology
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.

HY-133019

ATX inhibitor 5	Phosphodiesterase (PDE)	Inflammation/Immunology
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC₅₀ of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently.

HY-120088A

PF-06446846 hydrochloride	Ser/Thr Protease	Cardiovascular Disease
PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34.

HY-10440

Vismodegib GDC-0449	Hedgehog Autophagy	Cancer
Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, *ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

HY-114412

TD-0212	Angiotensin Receptor Neprilysin	Inflammation/Immunology Endocrinology
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT₁) antagonist and neprilysin (NEP) inhibitor, with a pK_i of 8.9 for AT₁ and a pIC₅₀ of 9.2 for NEP.

HY-100176

PF-4878691 3M-852A	Toll-like Receptor (TLR)	Infection Inflammation/Immunology
PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities.

HY-128554A

N-Desethyl amodiaquine dihydrochloride	Parasite	Infection
N-Desethyl amodiaquine dihydrochloride is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent. IC₅₀ values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively.

HY-106198

Lidorestat IDD-676	Aldose Reductase	Metabolic Disease
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC₅₀ of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation.

HY-111787

CSF1R-IN-2	Src c-Met/HGFR c-Fms	Cancer
CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC₅₀ values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

HY-18081

PF 750	FAAH Autophagy	Metabolic Disease
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC₅₀s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.

HY-19642

Glesatinib MGCD265	TAM Receptor c-Met/HGFR	Cancer
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

HY-B0725

Doxepin Hydrochloride	Histamine Receptor Cytochrome P450	Neurological Disease
Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and *1A2*.

HY-122700

Factor D inhibitor 6	Complement System	Inflammation/Immunology
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC₅₀ of 30 nM and a K_d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.

HY-100729A

GSK9311 hydrochloride	Epigenetic Reader Domain	Cancer
GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC₅₀ values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.

HY-N7000

Perillyl alcohol	Apoptosis Endogenous Metabolite	Cancer
Perillyl alcohol is a monoterpene isolated from the essential oils of lavendin, peppermint, spearmint, cherries, celery seeds, and several other plants. Perillyl alcohol is active in inducing apoptosis in tumor cells without affecting normal cells.

HY-109011

Rosiptor AQX-1125	Phosphatase	Cancer
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.

HY-131345

PI3Kα-IN-4
PI3K Cancer

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC₅₀ of 1.8 nM. PI3Kα-IN-4 has antitumor activity.

HY-B1190A

Cefadroxil hydrate BL-S 578 hydrate	Bacterial Antibiotic	Infection
Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.

HY-W008914

(E/Z)-CP-724714
EGFR Cancer

(E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor.

HY-19642A

Glesatinib hydrochloride MGCD265 hydrochloride	TAM Receptor c-Met/HGFR	Cancer
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

HY-135655

SPR720 disodium pVXc-486 disodium	Bacterial	Infection
SPR720 disodium (pVXc-486 disodium) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). SPR720 disodium has potent bactericidal activities in vivo.

HY-130248

BAY-899	Others	Endocrinology
BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC₅₀s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.

HY-106628

Sudoxicam	COX	Inflammation/Immunology
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.

HY-135829

BAY 2416964	Aryl Hydrocarbon Receptor	Cancer
BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC₅₀ of 341 nM. BAY 2416964 has the potential for solid tumors treatment.

HY-128554

N-Desethyl amodiaquine	Parasite	Infection
N-Desethyl amodiaquine is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine is an antiparasitic agent. IC₅₀ values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively.

HY-136142

Prasugrel chloride impurity	Others	Others
Prasugrel chloride impurity is a catp impurity of Prasugrel, exacted from patent US20130345428A1, line 0053. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.

HY-11083

GW-803430 GW-3430	MCHR1 (GPR24)	Metabolic Disease
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC₅₀ of 9.3. GW-803430 is orally active in an animal model of obesity.

HY-16759

Verubecestat MK-8931	Beta-secretase	Neurological Disease
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and *BACE2* inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.

HY-12279

Umbralisib TGR-1202; RP5264	PI3K	Cancer
Umbralisib (TGR-1202) is a novel *PI3Kδ* inhibitor, with IC₅₀ and EC₅₀ of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC₅₀ value of 6.0 μM.

HY-15319

AMG 487	CXCR	Cancer Inflammation/Immunology Endocrinology
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 *(CXCR3)* which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively.

HY-135221

Cefcapene pivoxil hydrochloride	Bacterial Antibiotic	Infection
Cefcapene pivoxil hydrochloride, an antibiotic, is an orally active and potent 3rd-generation cephalosporin with a wide spectrum of anti-bacterial activity.Cefcapene pivoxil hydrochloride has the potential for the palmoplantar pustulosis (PPP) treatment.

HY-16508

Ulipristal acetate CDB-2914	Progesterone Receptor Autophagy	Endocrinology Cancer
Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.

HY-N2411

Geissoschizine methyl ether	5-HT Receptor	Neurological Disease
Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is potent 5-HT_1A receptor agonist.

HY-133145A

hDDAH-1-IN-2 sulfate	Others	Cancer Inflammation/Immunology
hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.

HY-12033

2-Methoxyestradiol 2-ME2; NSC-659853	Apoptosis Microtubule/Tubulin Autophagy Endogenous Metabolite	Cancer
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.

HY-10787

Ximelagatran H 376/95	Thrombin	Cardiovascular Disease
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics.

HY-103018

Gusacitinib ASN-002	JAK Syk	Cancer
Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC₅₀ values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.

HY-N1673

2,5-Dihydroxybenzaldehyde Gentisaldehyde	Bacterial	Infection
2,5-Dihydroxybenzaldehyde (Gentisaldehyde) is a naturally occurring antimicrobial that inhibits the growth of *Mycobacterium avium subsp. paratuberculosis. 2,5-Dihydroxybenzaldehyde is active* against *S. aureus* strains with a MIC₅₀ of 500 mg/L.

HY-106409

Tefinostat CHR-2845	HDAC	Cancer
Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.

HY-100642

3-O-Methyltolcapone Ro 40-7591	COMT	Neurological Disease
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.

HY-12080

BX471 ZK-811752	CCR	Inflammation/Immunology Endocrinology
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a K_i of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

HY-110176

ASP2535
GlyT Neurological Disease

ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active