Search Result
Results for "
orally?bioavailable
" in MedChemExpress (MCE) Product Catalog:
30
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-114926
-
|
MAGL
|
Neurological Disease
|
KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells .
|
-
-
- HY-145479
-
|
PROTACs
Androgen Receptor
|
Cancer
|
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM .
|
-
-
- HY-19327
-
ACY-738
2 Publications Verification
|
HDAC
|
Cancer
|
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
|
-
-
- HY-128775
-
|
Others
|
Cancer
|
JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) proagent. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST .
|
-
-
- HY-146025
-
|
Others
|
Cancer
|
Antitumor agent-F10 (Compound F10) is a camptothecin derivative. Antitumor agent-F10 is an orally–bioavailable and potent antitumor agent. Antitumor agent-F10 displays lower acute toxicity than SN-38 does and the solubility of F10 reached 9.86 μg/mL .
|
-
-
- HY-B1149
-
-
-
- HY-B1149A
-
|
Bacterial
Antibiotic
|
Infection
|
Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
|
-
-
- HY-111485
-
-
-
- HY-119824
-
|
Bacterial
|
Cancer
|
Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity .
|
-
-
- HY-17630
-
-
-
- HY-114530
-
-
-
- HY-13017A
-
VX-770 benzenesulfonate
|
CFTR
Autophagy
|
Endocrinology
|
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
|
-
-
- HY-115874
-
|
CCR
|
Others
|
BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
|
-
-
- HY-145356
-
|
Others
|
Others
|
HbF inducer-1 is an orally bioavailable fetal hemoglobin inducer.
|
-
-
- HY-15604
-
-
-
- HY-12802
-
-
-
- HY-107986
-
-
-
- HY-15604A
-
-
-
- HY-100709
-
SL-01
|
|
|
ZPCK is an oral active proagent of gemcitabine that was designed for improved oral bioavailability .
|
-
-
- HY-76260
-
|
Bacterial
Antibiotic
|
Infection
|
Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.
|
-
-
- HY-112298
-
-
-
- HY-139885
-
|
c-Myc
|
Cancer
|
c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.
|
-
-
- HY-14178
-
|
ERK
|
Cancer
|
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
|
-
-
- HY-15968
-
GS-9973
|
Syk
|
Cancer
|
Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM.
|
-
-
- HY-19883
-
-
-
- HY-125879
-
-
-
- HY-13017B
-
VX-770 hydrate
|
CFTR
Autophagy
|
Endocrinology
|
Ivacaftor hydrate (VX-770 hydrate) is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
|
-
-
- HY-132901
-
|
SHP2
Phosphatase
|
Cancer
|
IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC50 value of 122 nM.
|
-
-
- HY-151805
-
|
MALT1
|
Cancer
|
RGT-068A is a potent, selective and oral bioavailable MALT1 inhibitor .
|
-
-
- HY-10480
-
-
-
- HY-16902
-
|
Syk
|
Inflammation/Immunology
|
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
|
-
-
- HY-100026
-
PQR620
3 Publications Verification
|
mTOR
|
Cancer
|
PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2 .
|
-
-
- HY-19809
-
-
-
- HY-16925
-
-
-
- HY-19984
-
|
CDK
|
Cancer
|
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
|
-
-
- HY-111486
-
-
-
- HY-139901
-
-
-
- HY-141895
-
|
PI3K
|
Cancer
|
Vps34-IN-3 is a potent, selective, and orally bioavailable VPS34 kinase inhibitor.
|
-
-
- HY-145354
-
-
-
- HY-122616
-
-
-
- HY-50911
-
FXR-450; XL335; WAY-362450
|
FXR
Autophagy
|
Metabolic Disease
Cancer
|
Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM .
|
-
-
- HY-17545
-
WNT974
|
Porcupine
|
Cancer
|
LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM .
|
-
-
- HY-102020
-
RG3039
1 Publications Verification
PF-06687859
|
Others
|
Neurological Disease
|
RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.
|
-
-
- HY-109004
-
BTA-C585
|
RSV
|
Infection
|
Enzaplatovir (BTA-C585) is an orally bioavailable Inhibitor for respiratory syncytial virus (RSV) infection .
|
-
-
- HY-112148
-
|
Akt
|
Cancer
|
AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1 .
|
-
-
- HY-135399
-
|
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-132900
-
|
ROR
|
Cancer
|
RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.
|
-
-
- HY-142214
-
|
TRP Channel
|
Others
|
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
|
-
-
- HY-14938
-
KCA 757; MN 001
|
Leukotriene Receptor
|
Inflammation/Immunology
|
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
|
-
-
- HY-15343
-
|
JAK
|
Cancer
|
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
|
-
- HY-16727
-
GS-5806
|
RSV
|
Infection
|
Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM .
|
-
- HY-100422
-
-
- HY-14419
-
|
mGluR
|
Neurological Disease
|
TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM .
|
-
- HY-105018
-
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-101820
-
|
EGFR
|
Cancer
|
Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-107978
-
-
- HY-117155
-
|
EGFR
|
Cancer
|
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM .
|
-
- HY-111500A
-
-
- HY-B0063
-
ST1481
|
Topoisomerase
|
Cancer
|
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity .
|
-
- HY-104059
-
-
- HY-101820A
-
|
EGFR
|
Cancer
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-W013331
-
|
Others
|
Inflammation/Immunology
|
Deoxy artemisinin, a orally bioavailable compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities .
|
-
- HY-16162A
-
|
TRP Channel
|
Cancer
|
D-3263 hydrochloride is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.
|
-
- HY-12353A
-
VX-787
|
Influenza Virus
|
Infection
|
Pimodivir (VX-787) is an orally bioavailable inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit.
|
-
- HY-109566
-
-
- HY-111484
-
SRN-927
|
Estrogen Receptor/ERR
|
Cancer
|
GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist .
|
-
- HY-128977
-
|
Epigenetic Reader Domain
|
Cancer
|
CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor .
|
-
- HY-107987
-
|
CXCR
|
Endocrinology
|
CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM .
|
-
- HY-112278
-
-
- HY-141845
-
|
LPL Receptor
|
Others
|
S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.
|
-
- HY-17536
-
KPT-330
|
CRM1
|
Cancer
|
Selinexor (KPT-330), analog of KPT-185, is an orally bioavailable and selective CRM1 inhibitor .
|
-
- HY-12300B
-
CFI-400945 fumarate
|
|
|
CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
|
-
- HY-12864
-
ARN-810; GDC-0810
|
Estrogen Receptor/ERR
|
Cancer
|
Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
|
-
- HY-B0729
-
Zinc L-carnosine
|
Others
|
Inflammation/Immunology
|
Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities.
|
-
- HY-112096
-
eCF506
2 Publications Verification
|
Src
|
Cancer
|
eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
|
-
- HY-112065
-
|
Sodium Channel
|
Metabolic Disease
|
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM .
|
-
- HY-112167A
-
ARRY-575 dihydrochloride; RG7741 dihydrochloride
|
Checkpoint Kinase (Chk)
|
Cancer
|
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
|
-
- HY-107363
-
|
mTOR
|
Cancer
|
FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.
|
-
- HY-131281
-
|
Drug Metabolite
|
Others
|
Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
|
-
- HY-131282
-
|
Drug Metabolite
|
Others
|
Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
|
-
- HY-132880
-
|
PI3K
|
Cancer
|
GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
|
-
- HY-139998
-
-
- HY-13301
-
|
HSP
|
Cancer
|
MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity .
|
-
- HY-13009
-
|
Acyltransferase
|
Metabolic Disease
|
PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC50 of 19 nM .
|
-
- HY-12528
-
-
- HY-15653
-
-
- HY-109565
-
ASTX660
|
IAP
Apoptosis
|
Cancer
|
Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-16997A
-
|
JAK
|
Cancer
|
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
|
-
- HY-13026S
-
CAL-101 d5; GS-1101 d5
|
PI3K
Autophagy
|
Cancer
|
Idelalisib-d5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor[1].
|
-
- HY-131283
-
|
Drug Metabolite
|
Endocrinology
|
8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
|
-
- HY-133127A
-
|
Glucokinase
|
Metabolic Disease
|
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity .
|
-
- HY-133127
-
|
Glucokinase
|
Metabolic Disease
|
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity .
|
-
- HY-114535
-
|
EGFR
|
Cancer
|
Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities .
|
-
- HY-141711
-
|
mAChR
|
Neurological Disease
|
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4 .
|
-
- HY-12300
-
CFI-400945 free base
|
Polo-like Kinase (PLK)
|
Cancer
|
CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
|
-
- HY-12045
-
HMN-214
4 Publications Verification
IVX-214
|
Polo-like Kinase (PLK)
|
Cancer
|
HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
|
-
- HY-50855B
-
CX-4945 sodium salt
|
Casein Kinase
Autophagy
|
Cancer
|
Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
|
-
- HY-18658
-
NVP-HDM201; HDM201
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
|
-
- HY-13467
-
-
- HY-112202
-
|
TRP Channel
|
Cardiovascular Disease
|
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4 .
|
-
- HY-14955
-
MB06322; CS-917
|
FBPase
|
Metabolic Disease
|
Managlinat dialanetil (MB06322) is an orally bioavailable inhibitor of fructose 1,6-bisphosphatase (FBPase) for the treatment of type 2 diabetes .
|
-
- HY-15656S
-
-
- HY-112712
-
|
HCV
|
Infection
|
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a .
|
-
- HY-114403
-
|
mGluR
|
Neurological Disease
|
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
|
-
- HY-15822
-
-
- HY-N4109
-
|
Others
|
Inflammation/Immunology
Cancer
|
Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity .
|
-
- HY-101869
-
MRK-409
|
GABA Receptor
|
Neurological Disease
|
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
|
-
- HY-19477
-
|
|
|
SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
|
-
- HY-139398
-
TBI-223
1 Publications Verification
|
Bacterial
|
Infection
|
TBI-223 is an orally bioavailable oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacterium tuberculosis (Mtb) .
|
-
- HY-14568
-
|
GlyT
|
Neurological Disease
|
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
|
-
- HY-19883S
-
-
- HY-114177A
-
(S)-PF-06873600
|
Others
|
Cancer
|
(S)-PF-06873600 it the S enantiomer of PF-06873600. PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK).
|
-
- HY-10633
-
|
TRP Channel
|
Neurological Disease
|
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
|
-
- HY-126137
-
-
- HY-122737
-
|
ROR
|
Inflammation/Immunology
|
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD .
|
-
- HY-112929
-
|
Phosphatase
|
Cancer
|
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
|
-
- HY-124669
-
|
Others
|
Cancer
|
RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability .
|
-
- HY-114245
-
Methylselenocysteine; Se-Methylseleno-L-cysteine
|
Apoptosis
Endogenous Metabolite
Beta-secretase
|
Cancer
|
Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis .
|
-
- HY-124600
-
|
HBV
|
Infection
|
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity .
|
-
- HY-145119
-
|
SARS-CoV
|
Infection
|
GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
|
-
- HY-128133
-
MMP8-I
|
MMP
|
Cancer
|
MMP-8 inhibitor-1 (compound 21), a hydroxamic acid derivative, is a potent MMP-8 inhibitor without significant oral bioavailability .
|
-
- HY-155088
-
|
mGluR
|
Metabolic Disease
|
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
|
-
- HY-114245B
-
Methylselenocysteine hydrochloride; Se-Methylseleno-L-cysteine hydrochloride
|
Endogenous Metabolite
Apoptosis
Beta-secretase
|
Cancer
|
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis .
|
-
- HY-125824
-
PF-06882961
|
GCGR
|
Metabolic Disease
|
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) .
|
-
- HY-163410
-
-
- HY-50709
-
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
|
-
- HY-15315
-
LY3009104; INCB028050
|
JAK
|
Inflammation/Immunology
|
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-15891
-
|
Elastase
|
Inflammation/Immunology
|
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM .
|
-
- HY-15891A
-
GW311616A
|
Elastase
|
Inflammation/Immunology
|
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM .
|
-
- HY-12870
-
|
Estrogen Receptor/ERR
|
Cancer
|
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-12870A
-
|
Estrogen Receptor/ERR
|
Cancer
|
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-15947A
-
GDC-0994 hydrochloride
|
ERK
|
Cancer
|
Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
|
-
- HY-101383
-
|
Sodium Channel
|
Neurological Disease
|
PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
|
-
- HY-103088
-
E7046
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities .
|
-
- HY-111050
-
|
c-Met/HGFR
|
Cancer
|
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
|
-
- HY-112305
-
|
ATM/ATR
|
Cancer
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-111498A
-
RGX-104
1 Publications Verification
Abequolixron
|
LXR
|
Inflammation/Immunology
Cancer
|
RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
|
-
- HY-100757
-
|
Histone Methyltransferase
|
Cancer
|
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
|
-
- HY-16640
-
|
JAK
|
Inflammation/Immunology
|
TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD) .
|
-
- HY-111390
-
|
Histone Methyltransferase
|
Cancer
|
Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
|
-
- HY-109055
-
E2609
|
Beta-secretase
|
Neurological Disease
|
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research .
|
-
- HY-114388
-
QM385
2 Publications Verification
|
Others
|
Inflammation/Immunology
|
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability .
|
-
- HY-133555
-
|
mGluR
|
Neurological Disease
|
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
|
-
- HY-131341
-
|
Syk
|
Inflammation/Immunology
Cancer
|
Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers .
|
-
- HY-14723
-
|
c-Met/HGFR
|
Cancer
|
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively .
|
-
- HY-144300
-
TNP-2198
|
Bacterial
|
Infection
|
Rifasutenizol (TNP-2198) is a potent and orally bioavailable dual-targeted antibacterial agent. Rifasutenizol has potent activity against microaerophilic and anaerobic bacterial pathogens .
|
-
- HY-15651A
-
AZD9668 tosylate
|
Elastase
|
Inflammation/Immunology
|
Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
|
-
- HY-50855
-
CX-4945
|
Casein Kinase
Autophagy
|
Cancer
|
Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
|
-
- HY-13245
-
INCB8761
|
CCR
|
Inflammation/Immunology
Endocrinology
|
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-15532B
-
MK-8776 S-isomer
|
Others
|
Cancer
|
SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
|
-
- HY-15315A
-
LY3009104 phosphate; INCB028050 phosphate
|
JAK
|
Inflammation/Immunology
|
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-18175
-
|
Checkpoint Kinase (Chk)
|
Cancer
|
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
|
-
- HY-111500
-
|
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-114411
-
|
Estrogen Receptor/ERR
|
Cancer
|
ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC50 of 40 nM .
|
-
- HY-131065
-
|
c-Met/HGFR
|
Cancer
|
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity .
|
-
- HY-145344
-
|
Phosphodiesterase (PDE)
|
Cancer
|
ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma .
|
-
- HY-151196
-
|
Others
|
Cardiovascular Disease
|
FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability .
|
-
- HY-149955
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%) .
|
-
- HY-124372
-
|
mGluR
|
Neurological Disease
|
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
|
-
- HY-161061
-
|
Arginase
|
Cancer
|
Arginase inhibitor 7 (compound A17) is an arginase (ARG1) inhibitor, with an IC50 of 0.16 μM. Arginase inhibitor 7 has high oral bioavailability .
|
-
- HY-16391A
-
PF-04449913 maleate
|
Smo
|
Cancer
|
Glasdegib maleate (PF-04449913 maleate) is a potent and orally bioavailable smoothened inhibitor. Glasdegib maleate binds to human SMO (amino acids 181-787) with IC50value of 4 nM .
|
-
- HY-15651
-
AZD9668
|
Elastase
|
Inflammation/Immunology
|
Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
|
-
- HY-16391
-
PF-04449913
|
Smo
|
Cancer
|
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
|
-
- HY-12340
-
|
PI3K
|
Cancer
|
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
|
-
- HY-16956
-
CC-223; ATG-008
|
mTOR
Apoptosis
|
Cancer
|
Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2.
|
-
- HY-11034
-
-
- HY-112286
-
|
PI3K
|
Inflammation/Immunology
|
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM .
|
-
- HY-128593
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH) .
|
-
- HY-B0689S
-
-
- HY-B1486
-
Ba 39089
|
|
|
Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .
|
-
- HY-139624
-
|
JNK
|
Others
|
JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
|
-
- HY-135399S
-
|
FXR
|
Inflammation/Immunology
|
Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid. Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
|
-
- HY-146223
-
|
Ras
|
Cancer
|
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-10758
-
|
Factor Xa
|
Cardiovascular Disease
|
FXa-IN-1 is a FXa inhibitor (IC50: 3 nM, Ki: 0.7 nM) with respectable oral bioavailability and half-life in vivo. FXa-IN-1 can be used for thromboembolic disorders .
|
-
- HY-10191
-
OSI-906
|
IGF-1R
Insulin Receptor
|
Endocrinology
Cancer
|
Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively .
|
-
- HY-12599
-
-
- HY-101842
-
|
Acetyl-CoA Carboxylase
|
Cancer
|
ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
|
-
- HY-111505
-
-
- HY-10244
-
|
HCV
|
Infection
|
MK-0608 is a potent and orally bioavailable inhibitor of HCV replication in vitro with an EC50 of 0.3 μM (EC90=1.3 μM) in the subgenomic-replicon assay .
|
-
- HY-12793
-
KPT-9274
|
PAK
NAMPT
|
Cancer
|
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively .
|
-
- HY-10480A
-
(R)-TAK-875
|
Others
|
Metabolic Disease
|
(R)-Fasiglifam is the isomer of Fasiglifam (HY-10480), and can be used as an experimental control. Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
|
-
- HY-14805
-
ST-246
|
Arenavirus
Orthopoxvirus
|
Infection
|
Tecovirimat(ST-246) is an orally bioavailable antipoxvirus compound; potent and selective active against multiple orthopoxviruses with EC50 about 10 nM. Tecovirimat could be used in the study for orthopoxvirus-induced diseases.
|
-
- HY-163081
-
|
PARP
|
Cancer
|
PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
|
-
- HY-157457
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research .
|
-
- HY-10302
-
|
CGRP Receptor
|
Neurological Disease
|
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
|
-
- HY-17001
-
|
Potassium Channel
iGluR
|
Neurological Disease
|
Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .
|
-
- HY-10422
-
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2 .
|
-
- HY-13592
-
Chidamide impurity
|
HDAC
|
Cancer
|
HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
|
-
- HY-15287
-
AG1341
|
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent .
|
-
- HY-107145
-
|
TAM Receptor
VEGFR
c-Met/HGFR
|
Cancer
|
Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
|
-
- HY-107145A
-
|
TAM Receptor
VEGFR
c-Met/HGFR
|
Cancer
|
Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
|
-
- HY-101789
-
|
Sodium Channel
|
Neurological Disease
|
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
|
-
- HY-N2593
-
|
Autophagy
|
Inflammation/Immunology
Cancer
|
Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation .
|
-
- HY-135230
-
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
|
-
- HY-15454
-
AT-406; Debio 1143; SM-406
|
IAP
Apoptosis
|
Cancer
|
Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
|
-
- HY-19483
-
|
|
|
ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.
|
-
- HY-139798
-
|
Bacterial
|
Infection
|
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice .
|
-
- HY-B1486A
-
Ba 39089 free base
|
|
|
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .
|
-
- HY-101340A
-
CFI-402257 hydrochloride
|
Mps1
|
Cancer
|
CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity .
|
-
- HY-13318
-
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-15287A
-
AG 1343 Mesylate
|
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent .
|
-
- HY-15531
-
Venetoclax
Maximum Cited Publications
123 Publications Verification
ABT-199; GDC-0199; RG7601
|
Bcl-2 Family
Autophagy
|
Cancer
|
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
|
-
- HY-13735A
-
Mepacrine dihydrochloride; SN-390 dihydrochloride
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Infection
Cancer
|
Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis .
|
-
- HY-106441A
-
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 Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
|
-
- HY-16751
-
-
- HY-13914
-
BAY 1000394
|
CDK
|
Cancer
|
Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.
|
-
- HY-133772
-
|
Drug Metabolite
|
Others
|
Venetoclax N-oxide is an impurity of Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM .
|
-
- HY-19558
-
|
|
|
IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM) .
|
-
- HY-141411A
-
(S)-MRI-1867
|
Cannabinoid Receptor
NO Synthase
|
Metabolic Disease
|
Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD) .
|
-
- HY-131952
-
-
- HY-18030B
-
|
Anaplastic lymphoma kinase (ALK)
|
Others
|
CEP-28122 mesylate hydrochloride is a diaminopyrimidine derivative.CEP-28122 mesylate hydrochloride is a potent, selective, and orally bioavailable ALK inhibitor with an IC50 of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor and good pharmacokinetic activity .
|
-
- HY-30237
-
Seliciclib; CYC202
|
CDK
|
Cancer
|
(R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
|
-
- HY-100626
-
|
Ser/Thr Protease
|
Cancer
|
WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively .
|
-
- HY-A0203
-
|
HIV
|
Infection
Inflammation/Immunology
|
Pentosan Polysulfate is an orally bioavailable medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate also displays a potent and selective anti-HIV activity. Pentosan Polysulfatecan be used for the research of interstitial cystitis .
|
-
- HY-100080
-
|
|
|
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo .
|
-
- HY-117900A
-
|
Btk
|
Inflammation/Immunology
|
(Rac)-PF-0625011 is a racemate of PF-06250112. PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor and shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC .
|
-
- HY-156698
-
|
PROTACs
|
Inflammation/Immunology
|
HJM-561 is a potent, selective, orally bioavailable EGFR PROTAC. HJM-561 overcomes osimertinib (HY-15772)-resistant EGFR triple mutations and has anti-tumor activity .
|
-
- HY-161014
-
|
DYRK
|
Cancer
|
DYRK2-IN-1 (Compd 54) is an orally bioavailable DYRK2 inhibitor, with an IC50 of 14 nM. DYRK2-IN-1 (Compd 54) can be used in the study of prostate cancer .
|
-
- HY-106755
-
BWA589C
|
HIV
|
Infection
Cancer
|
Tucaresol is an orally bioavailable immunopotentiatory drug that show to enhance T-helper-cell activity, with the induction of increased IL-2 and IFN-γ levels in mice and humans. Tucaresol has anti-HIV effect .
|
-
- HY-13017
-
VX-770
|
CFTR
Autophagy
|
Endocrinology
|
Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
|
-
- HY-18938
-
GS-4997
|
MAP3K
Apoptosis
|
Cancer
|
Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
|
-
- HY-102031
-
YY-20394
|
PI3K
|
Inflammation/Immunology
Cancer
|
Linperlisib (YY-20394) is a potent, orally bioavailable and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM .
|
-
- HY-15315S
-
LY3009104-d5; INCB028050-d5
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-15315S1
-
LY3009104-d3; INCB028050-d3
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-101930
-
|
11β-HSD
|
Metabolic Disease
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM .
|
-
- HY-112287
-
|
ERK
|
Cancer
|
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively .
|
-
- HY-108472
-
7-Allyl-8-oxoguanosine; RWJ 21757
|
Toll-like Receptor (TLR)
Influenza Virus
|
Infection
Cancer
|
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist .
|
-
- HY-105296
-
|
Sigma Receptor
mAChR
|
Cancer
|
Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
|
-
- HY-136146
-
|
nAChR
|
Neurological Disease
|
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
|
-
- HY-141866
-
|
Ceramidase
|
Neurological Disease
|
Acid Ceramidase-IN-1 is a potent and oral bioavailable acid ceramidase (AC, ASAH-1) inhibitor (hAC IC50=0.166 μM). Acid Ceramidase-IN-1 has excellent brain penetration in mice .
|
-
- HY-146075
-
|
Beta-lactamase
Bacterial
|
Infection
|
β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria .
|
-
- HY-120634
-
|
HCV
|
Infection
|
BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity .
|
-
- HY-149345
-
|
IRAK
|
Inflammation/Immunology
|
IRAK4-IN-24 (compound 16) is a potent IRAK4 inhibitor, with high clearance (Cl) and poor oral bioavailability. IRAK4-IN-24 can be used for research in inflammatory and autoimmune disorders.
|
-
- HY-17539
-
|
CRM1
|
Cancer
|
PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE). PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1 .
|
-
- HY-10038
-
DGAT-1 Inhibitor 4a
|
Acyltransferase
|
Metabolic Disease
|
A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
|
-
- HY-14291
-
LAF237; NVP-LAF 237
|
Dipeptidyl Peptidase
Ferroptosis
Apoptosis
|
Metabolic Disease
|
Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
|
-
- HY-15874
-
GSK2190915; AM-803
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
|
-
- HY-15874A
-
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
|
-
- HY-12681
-
|
Wnt
|
Cancer
|
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells . CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease .
|
-
- HY-15976
-
|
Others
|
Neurological Disease
|
P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease .
|
-
- HY-10290
-
|
Cathepsin
|
Metabolic Disease
|
MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S .
|
-
- HY-100761
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin .
|
-
- HY-A0203A
-
|
HIV
|
Infection
Inflammation/Immunology
|
Pentosan Polysulfate Sodium is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also is a potent and selective anti-HIV agent. Pentosan Polysulfate Sodium is used for the treatment of interstitial cystitis .
|
-
- HY-15463S
-
STI571-d8; CGP-57148B-d8
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
|
-
- HY-15463S1
-
STI571 d4; CGP-57148B d4
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
|
-
- HY-110176
-
|
GlyT
|
Neurological Disease
|
ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease .
|
-
- HY-131336
-
|
mGluR
|
Neurological Disease
|
MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia .
|
-
- HY-135891
-
|
CCR
|
Neurological Disease
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-120469
-
|
JAK
|
Inflammation/Immunology
|
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively .
|
-
- HY-102074
-
|
Others
|
Infection
|
ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency. .
|
-
- HY-144372
-
|
TRP Channel
|
Neurological Disease
|
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
|
-
- HY-146267
-
|
Estrogen Receptor/ERR
|
Cancer
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
|
-
- HY-147528
-
|
mGluR
|
Neurological Disease
|
mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic .
|
-
- HY-157332
-
|
Histone Methyltransferase
|
Cancer
|
WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazepinone-based WD repeat domain 5 (WDR5) inhibitor. WDR5-IN-7 can be used for the research of anti-cancer .
|
-
- HY-163300
-
-
- HY-15450A
-
|
CCR
|
Endocrinology
|
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
|
-
- HY-12861
-
|
p97
|
Cancer
|
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM .
|
-
- HY-P0025
-
(Melle-4)cyclosporin; SDZ NIM811
|
Mitochondrial Metabolism
HCV
|
Infection
Inflammation/Immunology
|
NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .
|
-
- HY-111457A
-
|
Elastase
|
Inflammation/Immunology
|
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
|
-
- HY-128596
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively .
|
-
- HY-107981
-
|
Antifolate
|
Cancer
|
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .
|
-
- HY-133149
-
|
Phospholipase
|
Cardiovascular Disease
|
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2) .
|
-
- HY-125415
-
|
PGE synthase
|
Inflammation/Immunology
|
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) .
|
-
- HY-134885
-
RM-023
|
SHP2
Ras
|
Cancer
|
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
|
-
- HY-124603
-
AT791
2 Publications Verification
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro .
|
-
- HY-120004
-
|
mAChR
|
Infection
|
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
|
-
- HY-10222
-
BMS-247550; Aza-epothilone B
|
Microtubule/Tubulin
Apoptosis
Bacterial
|
Cancer
|
Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
|
-
- HY-12113
-
ONX 0912; PR-047
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells .
|
-
- HY-111427
-
|
CDK
|
Cancer
|
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
|
-
- HY-120944
-
|
MMP
|
Inflammation/Immunology
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively .
|
-
- HY-B1486S
-
Ba 39089-d7
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
|
-
- HY-117900
-
|
Btk
|
Inflammation/Immunology
|
PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively .
|
-
- HY-N0447
-
-
- HY-119339
-
SX-682
4 Publications Verification
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .
|
-
- HY-15980
-
|
Parasite
|
Infection
|
GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
|
-
- HY-19614
-
|
|
|
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively .
|
-
- HY-108060
-
-
- HY-108060A
-
NM283 dihydrochloride
|
HCV
HCV Protease
Nucleoside Antimetabolite/Analog
|
Infection
|
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination .
|
-
- HY-122011
-
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration .
|
-
- HY-13245B
-
(Rac)-INCB8761
|
CCR
|
Inflammation/Immunology
|
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-50674
-
|
CCR
|
Inflammation/Immunology
Endocrinology
|
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
- HY-19981A
-
ARQ-087 Racemate
|
FGFR
|
Cancer
|
Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
|
-
- HY-100279
-
|
Antibiotic
|
Infection
Cancer
|
RMI 10874 is a tilorone analogue. Tilorone is a small-molecule, orally bioavailable antiviral agent. RMI 10874 completely abolishes lung colonization of an H-2 negative (GR9.B9) MCA-induced fibrosarcoma clone.
|
-
- HY-14291A
-
LAF237 dihydrate; NVP-LAF 237 dihydrate
|
Dipeptidyl Peptidase
Ferroptosis
Apoptosis
|
Metabolic Disease
|
Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity .
|
-
- HY-107457
-
|
mGluR
|
Neurological Disease
|
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
|
-
- HY-117650A
-
RG7834
3 Publications Verification
RO 7020322
|
HBV
|
Infection
|
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells .
|
-
- HY-15450
-
|
CCR
|
Endocrinology
|
INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
|
-
- HY-14364
-
|
Histamine Receptor
|
Inflammation/Immunology
|
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
|
-
- HY-148290
-
|
PROTACs
IRAK
|
Cancer
|
KTX-951 is a PROTAC targeting IRAK4 degradation (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential .
|
-
- HY-101699A
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
|
-
- HY-15532
-
MK-8776
|
Checkpoint Kinase (Chk)
|
Cancer
|
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .
|
-
- HY-15185
-
PF-3084014; PF-03084014
|
γ-secretase
Apoptosis
|
Cancer
|
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-15727
-
GSK2110183; LAE002
|
Akt
PKC
ROCK
|
Cancer
|
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively .
|
-
- HY-15727A
-
GSK2110183 hydrochloride; LAE002 hydrochloride
|
Akt
PKC
ROCK
|
Cancer
|
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively .
|
-
- HY-15590
-
AZ-23
3 Publications Verification
AZ23; AZ 23
|
Trk Receptor
|
Cancer
|
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
|
-
- HY-B1486AS
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
|
Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
|
-
- HY-129393
-
AB928
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities .
|
-
- HY-117604
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species .
|
-
- HY-107457A
-
|
mGluR
|
Neurological Disease
|
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes .
|
-
- HY-13318S
-
GS 4071-d3; Ro 64-0802-d3; Oseltamivir carboxylate-d3
|
Influenza Virus
|
Infection
|
Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, 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[1][2].
|
-
- HY-108646
-
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable .
|
-
- HY-15611
-
|
CRM1
|
Cancer
|
KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts .
|
-
- HY-161019
-
|
JAK
|
Inflammation/Immunology
|
JAK1/TYK2-IN-4 is a dual inhibitor of JAK and TYK2, with IC50s of 39 nM and 21 nM, respectively. JAK1/TYK2-IN-4 has oral bioavailability .
|
-
- HY-14434
-
BMS-650032
|
HCV
HCV Protease
SARS-CoV
|
Infection
|
Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM . Asunaprevir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-10619B
-
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-15043
-
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
|
-
- HY-50682
-
TTP488; PF-04494700
|
Amyloid-β
|
Neurological Disease
|
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD) . Azeliragon also can cross the blood-brain barrier (BBB) .
|
-
- HY-108677
-
|
Oxytocin Receptor
|
Endocrinology
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .
|
-
- HY-127105A
-
LNP023 hydrochloride
|
Complement System
Liposome
|
Metabolic Disease
Inflammation/Immunology
|
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
|
-
- HY-100678
-
|
Adenosine Receptor
PI3K
|
Inflammation/Immunology
Cancer
|
CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
|
-
- HY-100226
-
|
|
|
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases .
|
-
- HY-114147
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against agent-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability .
|
-
- HY-145341
-
|
Estrogen Receptor/ERR
|
Cancer
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
|
-
- HY-15546
-
|
CCR
|
Inflammation/Immunology
|
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .
|
-
- HY-15531S
-
ABT-199-d8; GDC-0199-d8; RG7601-d8
|
Bcl-2 Family
Autophagy
|
Cancer
|
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
|
-
- HY-141623
-
|
Others
|
Metabolic Disease
|
SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research .
|
-
- HY-155519
-
|
IRAK
|
Inflammation/Immunology
|
IRAK4-IN-26 (Compound 21) is a IRAK4 inhibitor (IC50: 6.2 nM). IRAK4-IN-26 displays an oral bioavailability of 21%. IRAK4-IN-26 can be used for research of inflammatory and autoimmune disorders .
|
-
- HY-114177
-
PF-06873600
|
CDK
|
Cancer
|
PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity .
|
-
- HY-19631A
-
NS-018
|
JAK
|
Cancer
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631B
-
NS-018 hydrochloride
|
JAK
|
Cancer
|
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631
-
NS-018 maleate
|
JAK
|
Cancer
|
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-128781
-
|
GCGR
|
Metabolic Disease
|
Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM) .
|
-
- HY-128353
-
|
ROR
|
Inflammation/Immunology
|
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5 .
|
-
- HY-109015S
-
Chidamide-d4; HBI-8000-d4; CS 055-d4
|
Isotope-Labeled Compounds
HDAC
|
Cancer
|
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
|
-
- HY-100886
-
|
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
|
-
- HY-132987
-
ARX-1796; AV-006
|
Beta-lactamase
Bacterial
|
Infection
|
Avibactam tomilopil (ARX-1796, AV-006), an Avibactam proagent, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes .
|
-
- HY-153715
-
Mitochondria modulator-1
|
Biochemical Assay Reagents
|
Metabolic Disease
|
Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
|
-
- HY-13847
-
|
mTOR
|
Cancer
|
GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
|
-
- HY-13026
-
CAL-101; GS-1101
|
PI3K
Autophagy
|
Cancer
|
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
|
-
- HY-14567
-
FUB-359
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-10619
-
MK-4827
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-15419
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-15289
-
FUB 359 maleate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-10619A
-
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10917
-
|
c-Fms
|
Inflammation/Immunology
Cancer
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-16976
-
|
Pim
|
Cancer
|
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma .
|
-
- HY-13323A
-
|
DNA/RNA Synthesis
|
Cancer
|
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
|
-
- HY-13213
-
AM211 free acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
|
-
- HY-119375
-
|
Bacterial
|
Infection
|
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively .
|
-
- HY-15185B
-
PF-3084014 dihydrobromide; PF-03084014 dihydrobromide
|
γ-secretase
Apoptosis
|
Cancer
|
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-105309
-
|
DYRK
|
Cardiovascular Disease
|
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia .
|
-
- HY-15419A
-
|
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-111515
-
|
Elastase
|
Inflammation/Immunology
|
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
|
-
- HY-125856
-
BMS-986177; JNJ-70033093
|
Factor Xa
|
Cardiovascular Disease
|
Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study .
|
-
- HY-145928
-
GDC-6036
|
Ras
|
Cancer
|
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
|
-
- HY-10619E
-
MK-4827 tosylate hydrate
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-145119S
-
JT001 free base; VV116 free base; GS-621763-d1
|
Isotope-Labeled Compounds
|
Others
|
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
|
-
- HY-156703S
-
|
HBV
|
Infection
|
HBV-IN-39-d3 (Example 14) is a deuterated HBV-IN-39 (Example 13). HBV-IN-39 is an HBV inhibitor. HBV-IN-39-d3 has better oral bioavailability than HBV-IN-39 .
|
-
- HY-116625
-
|
GHSR
|
Neurological Disease
|
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research .
|
-
- HY-109142
-
AK0529; RO-0529
|
RSV
|
Infection
|
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species .
|
-
- HY-14291S1
-
-
- HY-10096
-
|
GSK-3
|
Neurological Disease
|
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
|
-
- HY-156593
-
|
ROCK
|
Cancer
|
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
|
-
- HY-13245A
-
(s)-INCB8761
|
Others
|
Inflammation/Immunology
Endocrinology
|
(s)-PF-4136309 is the isomer of PF-4136309 (HY-13245), and can be used as an experimental control. PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-109042
-
CORT 125134
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
|
-
- HY-15245
-
|
PI3K
|
Cancer
|
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
- HY-14291S
-
-
- HY-103696
-
|
Apoptosis
|
Cancer
|
PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis .
|
-
- HY-145311
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer .
|
-
- HY-144858
-
EZM0414
3 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma .
|
-
- HY-139970
-
|
Androgen Receptor
|
Endocrinology
Cancer
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
|
-
- HY-119272
-
|
ERK
Caspase
|
Cancer
|
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
|
-
- HY-145844
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers .
|
-
- HY-15970
-
KPT-335
|
CRM1
|
Cancer
|
Verdinexor(KPT-335) is a novel, orally bioavailable selective inhibitor of nuclear export (SINE), inhibits nuclear export protein Exportin 1(XPO1/CRM1) against canine tumor cell lines; also reduce influenza virus replication in vitro and in vivo.
|
-
- HY-111187
-
KX-02
|
Src
Microtubule/Tubulin
Apoptosis
|
Cancer
|
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell .
|
-
- HY-15010
-
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
|
-
- HY-16125
-
L-651582 Orotate; CAI Orotate
|
Calcium Channel
|
Inflammation/Immunology
Cancer
|
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects .
|
-
- HY-107365
-
|
PI3K
mTOR
|
Cancer
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
|
-
- HY-124283A
-
|
Cannabinoid Receptor
|
Neurological Disease
|
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors .
|
-
- HY-132298
-
|
Adenylate Cyclase
|
Others
|
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound .
|
-
- HY-151625
-
|
PARP
Apoptosis
|
Cancer
|
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
|
-
- HY-13017S2
-
VX-770-d18
|
Autophagy
CFTR
|
Endocrinology
|
Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
|
-
- HY-145928B
-
GDC-6036 adipate
|
Ras
|
Cancer
|
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .
|
-
- HY-14466
-
|
Prostaglandin Receptor
|
Endocrinology
|
GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain .
|
-
- HY-10864
-
URB-597
4 Publications Verification
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
|
-
- HY-10300
-
SCH 900518
|
HCV
HCV Protease
SARS-CoV
|
Infection
|
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease . Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM .
|
-
- HY-10237
-
EBP 520; SCH 503034
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-13491
-
|
Trk Receptor
|
Cancer
|
GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
|
-
- HY-18204A
-
LCZ696
|
Angiotensin Receptor
Neprilysin
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure . Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis .
|
-
- HY-18030A
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity .
|
-
- HY-104037
-
LYC-55716
|
ROR
|
Cancer
|
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
|
-
- HY-15287S
-
|
Isotope-Labeled Compounds
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
|
-
- HY-124596
-
NKR-P1A
|
Epigenetic Reader Domain
|
Cancer
|
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .
|
-
- HY-120028
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells .
|
-
- HY-111457
-
|
Others
|
Inflammation/Immunology
|
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM . BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC) .
|
-
- HY-127105
-
LNP023
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
|
-
- HY-16434
-
|
Acyltransferase
|
Metabolic Disease
|
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome .
|
-
- HY-50674A
-
|
CCR
|
Inflammation/Immunology
|
INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity .
|
-
- HY-132292
-
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
|
-
- HY-145835
-
|
PERK
|
Cancer
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-B0497S1
-
BAY2353-13C6
|
Isotope-Labeled Compounds
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
|
-
- HY-151360
-
|
Sodium Channel
|
Metabolic Disease
|
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
|
-
- HY-15785
-
TAS-116
|
HSP
|
Cancer
|
Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
|
-
- HY-126321
-
|
ROR
|
Cancer
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
|
-
- HY-19867A
-
TG-0054 hydrobromide
|
CXCR
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization . Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction .
|
-
- HY-133129
-
MS1943
1 Publications Verification
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines .
|
-
- HY-135853
-
EIDD-2801; MK-4482
|
SARS-CoV
Influenza Virus
|
Infection
|
Molnupiravir (EIDD-2801) is an orally bioavailable proagent of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza .
|
-
- HY-122559
-
|
mGluR
|
Neurological Disease
|
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
|
-
- HY-122058A
-
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
|
-
- HY-132189
-
R101933
|
P-glycoprotein
|
Cancer
|
Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters . Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) . Laniquidar has limited oral bioavailability .
|
-
- HY-15023
-
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .
|
-
- HY-14291B
-
(2R)-LAF237; (2R)-NVP-LAF 237
|
Others
|
Metabolic Disease
|
(2R)-Vildagliptin is the isomer of Vildagliptin (HY-14291), and can be used as an experimental control. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
|
-
- HY-15445
-
CTEP
2 Publications Verification
RO 4956371; mGluR5 inhibitor
|
mGluR
|
Neurological Disease
|
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17377
-
SCH-417690 maleate; SCH-D maleate
|
CCR
HIV
|
Infection
Endocrinology
|
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
|
-
- HY-15656
-
LDK378
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
|
-
- HY-15656A
-
LDK378 dihydrochloride
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
|
-
- HY-15959
-
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
|
-
- HY-17593
-
CEM-101; OP-1068
|
Bacterial
Antibiotic
|
Infection
|
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
|
-
- HY-133552
-
|
ROR
|
Inflammation/Immunology
|
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
|
-
- HY-112601
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively . Anticancer activity .
|
-
- HY-114277
-
AMG-510
|
Ras
|
Cancer
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors .
|
-
- HY-111925
-
|
TRP Channel
|
Cardiovascular Disease
|
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
|
-
- HY-103104
-
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
|
-
- HY-106003
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
Inflammation/Immunology
|
GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects .
|
-
- HY-124593
-
PTC299
1 Publications Verification
|
VEGFR
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Cancer
|
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies .
|
-
- HY-145695
-
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
|
-
- HY-157838
-
|
MAP4K
|
Cancer
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
|
-
- HY-B0717
-
TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS
|
Others
|
Neurological Disease
Metabolic Disease
|
Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E .
|
-
- HY-101761
-
|
PAI-1
Apoptosis
|
Cancer
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-10847A
-
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-130119
-
|
Integrin
|
Cancer
|
Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively .
|
-
- HY-128345
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP) .
|
-
- HY-116000
-
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-117853
-
ABT-761; VIA-2291
|
Lipoxygenase
|
Cardiovascular Disease
|
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation . Atreleuton is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-107676
-
|
nAChR
|
Neurological Disease
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders .
|
-
- HY-133119
-
|
Bacterial
|
Infection
|
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively .
|
-
- HY-144393
-
|
BCRP
|
Cancer
|
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .
|
-
- HY-110117
-
|
Integrin
Interleukin Related
|
Inflammation/Immunology
|
BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders .
|
-
- HY-77111
-
|
Others
|
Inflammation/Immunology
Endocrinology
|
cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
- HY-146223A
-
|
Others
|
Cancer
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-10917S
-
|
Isotope-Labeled Compounds
c-Fms
|
Inflammation/Immunology
Cancer
|
GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-10206
-
MP470; HPK 56
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-109015
-
Chidamide; HBI-8000; CS 055
|
HDAC
|
Cancer
|
Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 .
|
-
- HY-18161
-
|
FLT3
Aurora Kinase
|
Cancer
|
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
|
-
- HY-10237S
-
EBP 520-d9; SCH 503034-d9
|
Isotope-Labeled Compounds
HCV Protease
HCV
SARS-CoV
|
Infection
|
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
|
-
- HY-125858
-
MI-1061
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-12168
-
BAY 12-9566
|
MMP
|
Cancer
|
Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
|
-
- HY-10206A
-
MP470 hydrochloride; HPK 56 hydrochloride
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
|
Cancer
|
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-50887
-
|
Cathepsin
|
Metabolic Disease
|
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively . L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption .
|
-
- HY-125836
-
|
CCR
|
Endocrinology
Cancer
|
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
|
-
- HY-129707
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents .
|
-
- HY-150080
-
BMS-986180
|
HIV
HIV Integrase
|
Infection
|
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
|
-
- HY-151813
-
|
Others
|
Cancer
|
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
|
-
- HY-101761A
-
|
PAI-1
Apoptosis
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-50878
-
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-15463
-
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
|
-
- HY-124634
-
PZ-2891
1 Publications Verification
|
Others
|
Neurological Disease
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
|
-
- HY-109118A
-
SUVN-502 mesylate
|
5-HT Receptor
|
Neurological Disease
|
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
|
-
- HY-125858A
-
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-142160
-
|
Raf
|
Cancer
|
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
|
-
- HY-116804
-
|
Histone Methyltransferase
|
Cancer
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-133747
-
|
JAK
|
Inflammation/Immunology
|
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research .
|
-
- HY-151424
-
|
Proteasome
|
Cancer
|
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
|
-
- HY-135853S
-
EIDD-2801-d7; MK-4482-d7
|
SARS-CoV
Influenza Virus
|
Inflammation/Immunology
|
Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza[1][2].
|
-
- HY-50878B
-
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-157442
-
|
Salt-inducible Kinase (SIK)
|
Inflammation/Immunology
|
GLPG3312 (Compound 28) is a selective pan-SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases .
|
-
- HY-15463S2
-
STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
|
Autophagy
Bcr-Abl
c-Kit
SARS-CoV
PDGFR
|
Cancer
|
Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-110160
-
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
|
-
- HY-128570
-
|
Complement System
|
Inflammation/Immunology
|
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively .
|
-
- HY-144256
-
|
Others
|
Cancer
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
|
-
- HY-146388
-
|
Bacterial
ATP Synthase
|
Infection
|
Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium .
|
-
- HY-163407
-
|
Galectin
|
Cancer
|
Galectin-3-IN-4 (compound 5) is a carboxamide analog. Galectin-3-IN-4 is a potent, selective, and orally bioavailable inhibitor of human and mouse galectin-3, with IC50 values of 21 and 167 nM for hGal-3 and mGal-3, respectively. Galectin-3-IN-4 has IC50 values of 1580 and 2750 nM for hGal-1 and hGal-9, respectively .
|
-
- HY-14483
-
AF-353
1 Publications Verification
Ro-4
|
P2X Receptor
|
Cancer
|
AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3 .
|
-
- HY-101855
-
Anle138b
|
Amyloid-β
|
Neurological Disease
|
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
|
-
- HY-N2510
-
Myristicine
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
|
-
- HY-131275
-
|
Drug Metabolite
|
Others
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
|
-
- HY-145594
-
AB-291; DS-1001
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively .
|
-
- HY-12168B
-
(Rac)-BAY 12-9566
|
MMP
|
Cancer
|
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
|
-
- HY-10209
-
AB1010
|
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-12010
-
AC480 Hydrochloride
|
EGFR
|
Cancer
|
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-10209A
-
AB-1010 mesylate
|
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-12868
-
PQR309
|
PI3K
mTOR
|
Cancer
|
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
|
-
- HY-15823
-
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.
CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM) .
|
-
- HY-50878S
-
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-13836
-
|
Parasite
|
Infection
|
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial .
|
-
- HY-128879A
-
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
|
-
- HY-105685
-
|
Vasopressin Receptor
|
Neurological Disease
|
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .
|
-
- HY-10251
-
AC480
|
EGFR
|
Cancer
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-128879
-
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
|
-
- HY-109118
-
SUVN-502 free base
|
5-HT Receptor
|
Neurological Disease
|
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
|
-
- HY-120124
-
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
|
-
- HY-146789
-
|
PI3K
|
Cancer
|
PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
|
-
- HY-146057
-
|
Bacterial
|
Infection
|
Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
|
-
- HY-155416
-
|
SARS-CoV
|
Infection
|
M56-S2 iodide is a SARS-CoV-2 M pro inhibitor (IC50=4.0 μM). M56-S2 iodide showed good oral bioavailability and low toxicity in ADMET prediction. M56-S2 iodide has good drug potential and can be used in antiviral (such as SARS-CoV-2) research .
|
-
- HY-50878A
-
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-101117
-
|
Histone Methyltransferase
|
Cancer
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- HY-109035
-
SB9200; GS-9992
|
HCV
HBV
|
Infection
|
Inarigivir soproxil (SB9200) is an agonist of innate immunity and shows potent antiviral activity against resistant HCV variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems. Inarigivir soproxil, an orally bioavailable proagent of SB 9000, has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, respiratory syncytial virus and influenza and HBV .
|
-
- HY-126750
-
GNF362
1 Publications Verification
|
Phosphatase
|
Inflammation/Immunology
|
GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4] .
|
-
- HY-16361A
-
CGP3466B; CGP3446 maleate; TCH346 maleate
|
|
|
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease . Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD) . Omigapil (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14979A
-
|
Raf
Bcr-Abl
Discoidin Domain Receptor
VEGFR
RET
Ephrin Receptor
|
Cancer
|
ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers .
|
-
- HY-123857
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .
|
-
- HY-14291S2
-
LAF237-13C5,15N; NVP-LAF 237-13C5,15N
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
|
-
- HY-12501A
-
ITI-214
3 Publications Verification
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
|
-
- HY-16961
-
MGCD516; MG-516
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
- HY-117287
-
BMS-986165
|
JAK
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
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-
- HY-16961A
-
MGCD516 malate; MG-516 malate
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
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-
- HY-112602
-
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively . Antitumor activity .
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-
- HY-122608
-
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
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-
- HY-13208
-
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
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-
- HY-143880
-
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
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- HY-141431
-
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .
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-
- HY-148825
-
-
- HY-13265
-
AR-42
2 Publications Verification
HDAC-42; OSU-HDAC42
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
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-
- HY-13246
-
GDC-0980; GNE 390; RG 7422
|
PI3K
mTOR
Apoptosis
|
Cancer
|
Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
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- HY-15514A
-
LY2801653 dihydrochloride
|
c-Met/HGFR
FLT3
ROS Kinase
Discoidin Domain Receptor
|
Cancer
|
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
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- HY-13967B
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents . AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-12501
-
|
Phosphodiesterase (PDE)
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Neurological Disease
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
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-
- HY-100014
-
|
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) .
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- HY-100370
-
|
GABA Receptor
|
Cancer
|
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
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-
- HY-100818
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TAS-120
|
FGFR
|
Cancer
|
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
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-
- HY-112306
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DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
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-
- HY-126291
-
|
Sodium Channel
|
Neurological Disease
|
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively .
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-
- HY-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
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-
- HY-144122
-
|
HIV
|
Infection
|
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
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-
- HY-15514
-
LY2801653
|
c-Met/HGFR
FLT3
ROS Kinase
Discoidin Domain Receptor
|
Cancer
|
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
|
-
- HY-12169
-
BB2516; TA2516
|
MMP
|
Cancer
|
Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes .
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-
- HY-135985
-
|
Others
|
Cancer
|
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-120184
-
AZ13713945
|
mAChR
|
Neurological Disease
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
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-
- HY-120878
-
|
CXCR
|
Inflammation/Immunology
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM .
|
-
- HY-138563
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
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-
- HY-100555
-
|
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
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-
- HY-151535
-
|
SARS-CoV
|
Infection
Inflammation/Immunology
|
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
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-
- HY-125858B
-
|
Others
|
Others
|
(S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-13270
-
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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-
- HY-13238
-
S/GSK1349572
|
HIV Integrase
HIV
|
Infection
|
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
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-
- HY-124322
-
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
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-
- HY-123960A
-
|
Phosphatase
|
Neurological Disease
|
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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-
- HY-123960
-
|
Phosphatase
|
Neurological Disease
|
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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-
- HY-13238A
-
S/GSK1349572 sodium
|
HIV Integrase
HIV
|
Infection
|
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
- HY-14362
-
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
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-
- HY-15724
-
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
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-
- HY-10847B
-
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
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-
- HY-15724A
-
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
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-
- HY-13238S1
-
S/GSK1349572-d3
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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-
- HY-13238S2
-
S/GSK1349572-d5
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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-
- HY-13342AS
-
YN968D1-d8 free base
|
Src
VEGFR
Autophagy
c-Kit
RET
|
Cancer
|
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
|
-
- HY-19974
-
TAK-220
2 Publications Verification
|
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.
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-
-
-
HY-L061
-
|
3489 compounds
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3489 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
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-
-
HY-L0121V
-
|
10,000 compounds
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
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-
-
HY-L902
-
|
5000 compounds
|
MCE 5K Scaffold Library consists of 5,000 lead-like compounds. Each compound represents one unique scaffold. All compounds are compatible with Lipinski’s rule (Rule of 5) with multiple characteristics such as calculated good solubility (-3.2<logP<5), oral bioavailability (RotB<=10), drug transportability (PSA<120). Compounds contained within the library have been screened to remove any inappropriate chemical structures, avoiding “false hits”. The sufficient diverse of compound structure makes this library a powerful tool for drug screening.
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-
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HY-L901
-
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50000 compounds
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MCE 50K Diversity Library consists of 50,000 lead-like compounds with multiple characteristics such as calculated good solubility (-3.2<logP<5), oral bioavailability (RotB<=10), drug transportability (PSA<120). These compounds were selected by dissimilarity search with an average Tanimoto Coefficient of 0.52. There are 36,857 unique scaffolds and each scaffold 1 to 7 compounds. What’s more, compounds with the same scaffold have as many functional groups as possible, which make abundant chemical spaces. This exceptionally diverse library is highly recommended for random screening against new as well as popular targets based its novel, diverse scaffolds, abundant chemical spaces and the convenience for subsequent modification.
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Cat. No. |
Product Name |
Target |
Research Area |
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-13026S
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Idelalisib-d5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor[1].
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- HY-15656S
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Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
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- HY-19883S
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Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
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- HY-B0689S
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Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
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- HY-135399S
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Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid. Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
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- HY-15315S
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Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
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- HY-15315S1
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Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
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- HY-15463S
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1 Publications Verification
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Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
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- HY-15463S1
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Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
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- HY-B1486S
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Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
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- HY-B1486AS
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Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
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- HY-13318S
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Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, 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[1][2].
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- HY-15531S
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Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
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- HY-109015S
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Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
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- HY-145119S
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GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
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- HY-156703S
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HBV-IN-39-d3 (Example 14) is a deuterated HBV-IN-39 (Example 13). HBV-IN-39 is an HBV inhibitor. HBV-IN-39-d3 has better oral bioavailability than HBV-IN-39 .
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- HY-14291S1
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Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
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- HY-14291S
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Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1][2].
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- HY-13017S2
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Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
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- HY-15287S
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Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
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- HY-B0497S1
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Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
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- HY-10917S
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GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
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- HY-10237S
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Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
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- HY-135853S
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Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza[1][2].
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- HY-15463S2
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Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
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- HY-50878S
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Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
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- HY-14291S2
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Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
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- HY-13238S1
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Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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- HY-13238S2
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Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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- HY-13342AS
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Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
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Cat. No. |
Product Name |
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Classification |
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- HY-10533
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5-Ethynyluracil; GW776C85
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Alkynes
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Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil) . Eniluracil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-16247
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HE3235
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Alkynes
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Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer . Apoptone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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