Search Result
Results for "5-ht1E Receptors Inhibitors" in MCE Product Catalog:
9670
Inhibitors & Agonists
10
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-13221
-
-
- HY-U00439
-
-
- HY-131005
-
-
- HY-121879
-
-
- HY-75502
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-19373
-
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P2519
-
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-N7247
-
|
Thiochrome
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
|
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-P2518
-
-
- HY-B0649
-
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-110303
-
-
- HY-B1510S
-
-
- HY-126941
-
|
Hecogenin acetate
|
Opioid Receptor
|
Neurological Disease
|
|
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
|
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-13418A
-
|
Dorsomorphin
Compound C; BML-275
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
|
-
- HY-B1478
-
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-18728
-
-
- HY-14415
-
|
SR8278
|
Others
|
Metabolic Disease
|
|
SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
|
-
- HY-P1329
-
-
- HY-P1329A
-
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-13418
-
|
Dorsomorphin dihydrochloride
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
|
-
- HY-P1335
-
|
CTAP
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-N0050
-
|
Allomatrine
(+)-Allomatrine
|
Others
|
Neurological Disease
|
|
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
|
-
- HY-P1335A
-
|
CTAP TFA
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-101348
-
-
- HY-B0098S
-
-
- HY-B1494
-
-
- HY-101372A
-
|
Oxotremorine M iodide
|
mAChR
|
Neurological Disease
|
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
|
-
- HY-129995A
-
-
- HY-15583
-
-
- HY-128113
-
-
- HY-12206
-
|
Thioperamide
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
|
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-13728
-
|
Plevitrexed
ZD 9331; BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
|
-
- HY-135588
-
-
- HY-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-15404
-
|
Darusentan
Lu-135252
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM.
|
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-W040146
-
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-108847
-
|
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-18200
-
|
Atopaxar
E5555; ER-172594-00
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
|
-
- HY-101299A
-
|
Dihydrexidine
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.
|
-
- HY-101299B
-
|
Dihydrexidine hydrochloride
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.
|
-
- HY-14325
-
|
L-745870
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-14325B
-
|
L-745870 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-108057A
-
|
Facinicline hydrochloride
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
|
-
- HY-100348
-
|
EPI-001
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo.
|
-
- HY-42849
-
-
- HY-42849A
-
-
- HY-17497S
-
-
- HY-11052A
-
|
Trap-101 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
|
-
- HY-12237
-
-
- HY-10847A
-
|
SB-277011 dihydrochloride
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-14551
-
-
- HY-115613
-
|
ML-180
SR1848
|
Others
|
Cancer
|
|
ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.
|
-
- HY-133189
-
-
- HY-13965
-
|
Parmodulin 2
ML161
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
|
-
- HY-14648
-
-
- HY-P1302
-
|
Orphanin FQ(1-11)
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.
|
-
- HY-N6932
-
-
- HY-15319
-
-
- HY-90010
-
|
Tolterodine tartrate
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
|
|
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-103187
-
-
- HY-P1302A
-
|
Orphanin FQ(1-11) TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.
|
-
- HY-W001909
-
|
Myosmine
|
nAChR
|
Metabolic Disease
|
|
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.
|
-
- HY-70002B
-
-
- HY-P1313A
-
-
- HY-103200
-
-
- HY-100672
-
-
- HY-103568
-
|
YM-298198 hydrochloride
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
|
-
- HY-103090
-
-
- HY-P2497
-
-
- HY-133113
-
-
- HY-P1345
-
|
TLQP-21
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-100369A
-
|
DMCM hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
|
-
- HY-P1345A
-
|
TLQP-21 TFA
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-B0589C
-
|
(3S,5S)-Atorvastatin
|
Cytochrome P450
|
Metabolic Disease
|
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-112055
-
|
DIM-C-pPhOH
|
Apoptosis
|
Cancer
|
|
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
|
-
- HY-14249
-
-
- HY-100634
-
|
4-Hydroxypropranolol hydrochloride
(±)-4-hydroxy Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-110278
-
|
ADX71743
|
mGluR
|
Neurological Disease
|
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
|
-
- HY-N7272
-
|
Cirsimarin
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase.
|
-
- HY-135147
-
|
ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-70081A
-
|
Sumanirole maleate
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.
|
-
- HY-P1471
-
-
- HY-P2287
-
|
Cortagine
|
CRFR
|
Neurological Disease
|
|
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
|
-
- HY-133045
-
|
VHL Ligand 8
|
Ligand for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-N7707
-
|
Sandacanol
|
Apoptosis
|
Cancer
|
|
Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
|
-
- HY-121538
-
|
CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-A0036
-
|
Bazedoxifene acetate
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
-
- HY-P1112
-
-
- HY-19434A
-
|
cis-ACPD
|
iGluR
mGluR
|
Neurological Disease
|
|
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. And it is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
|
-
- HY-P1471A
-
|
Adrenomedullin (AM) (22-52), human TFA
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
|
-
- HY-136208
-
|
TAN-452
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
|
-
- HY-P1112A
-
-
- HY-A0031
-
|
Bazedoxifene
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
-
- HY-A0031A
-
|
Bazedoxifene hydrochloride
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
-
- HY-100991
-
|
FG 7142
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
|
-
- HY-19608
-
-
- HY-14903
-
|
Ulimorelin
TZP-101
|
GHSR
Adrenergic Receptor
|
Metabolic Disease
|
|
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
|
-
- HY-U00387
-
-
- HY-100634S
-
|
4-Hydroxypropranolol D7 hydrochloride
(±)-4-hydroxy Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-108495
-
|
CYM50308
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
|
-
- HY-P1338
-
|
PL-017
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats.
|
-
- HY-100234A
-
-
- HY-100234
-
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-P1338A
-
|
PL-017 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.
|
-
- HY-14569
-
|
CDPPB
|
mGluR
|
Neurological Disease
|
|
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
|
-
- HY-12598
-
|
(S)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.
|
-
- HY-110160
-
|
Pozanicline dihydrochloride
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-113313
-
|
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
|
-
- HY-107380A
-
|
PGlu-3-methyl-His-Pro-NH2 TFA
A-42872 TFA
|
Others
|
Endocrinology
|
|
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-133044
-
|
Boc-Pip-alkyne-Ph-COOH
|
PROTAC Linker
|
Cancer
|
|
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-110237
-
|
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-106244A
-
|
DOTATATE acetate
|
Others
|
Cancer
|
|
DOTATATE acetate, a DOTA-conjugated peptide, and can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).
|
-
- HY-10121
-
|
Asenapine
Org 5222
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Asenapine is an antagonist of serotonin receptors (5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7), adrenoceptors (α1, α2A, α2B, α2C), dopamine receptors (D2, D3, D4) and histamine receptors (H 1, H2), with pKis of 8.4-10.5, 8.9-9.5, 8.9-9.4 and 8.2-9.0, respectively. Asenapine has antipsychotic activity, can be used in the research of schizophrenia and bipolar disorder.
|
-
- HY-112720
-
-
- HY-76569
-
|
Desfesoterodine
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
|
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
|
-
- HY-A0030
-
|
Fesoterodine fumarate
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).
|
-
- HY-70053
-
|
Fesoterodine
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB).
|
-
- HY-124733A
-
-
- HY-133073
-
|
CCR7 Ligand 1
CCR7-Cmp2105
|
CCR
Ligand for Target Protein for PROTAC
|
Cancer
|
|
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
|
-
- HY-135303
-
|
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-70053A
-
|
Fesoterodine L-mandelate
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).
|
-
- HY-16489A
-
|
Terodiline hydrochloride
|
mAChR
Calcium Channel
|
Neurological Disease
|
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.
|
-
- HY-116330A
-
|
Hyperforin dicyclohexylammonium salt
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
|
-
- HY-108625
-
|
SHA 68
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
|
-
- HY-103476
-
|
Ro15-4513
|
GABA Receptor
|
Neurological Disease
|
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
|
-
- HY-100371
-
|
(RS)-MCPG
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-B0160
-
-
- HY-12949
-
|
ML204
|
TRP Channel
|
Neurological Disease
|
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-12949A
-
|
ML204 hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-136209
-
|
SU5208
|
VEGFR
|
Cancer
|
|
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2).
|
-
- HY-50675
-
-
- HY-13276
-
-
- HY-B0407AS
-
-
- HY-N2003
-
|
D-Tetrahydropalmatine
|
Dopamine Receptor
|
Metabolic Disease
|
|
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
|
-
- HY-B2070
-
-
- HY-U00313
-
-
- HY-103244
-
|
CITCO
|
Apoptosis
|
Cancer
|
|
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
|
-
- HY-N0835
-
-
- HY-B0327A
-
-
- HY-B0327
-
-
- HY-101957
-
|
AG 1295
|
PDGFR
|
Cardiovascular Disease
|
|
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P1260
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-P1319
-
|
Nociceptin(1-7)
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
|
-
- HY-19815
-
-
- HY-101091
-
-
- HY-100019
-
|
Rogaratinib
BAY1163877
|
FGFR
|
Cancer
|
|
Rogaratinib is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor.
|
-
- HY-15371
-
|
Forskolin
Coleonol; Colforsin
|
Adenylate Cyclase
FXR
Autophagy
|
Cancer
Endocrinology
Metabolic Disease
Inflammation/Immunology
|
|
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
|
-
- HY-100714A
-
|
D-AP5
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
|
-
- HY-101653
-
|
MHP 133
|
AChE
mAChR
5-HT Receptor
|
Neurological Disease
|
|
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
|
-
- HY-P1260A
-
-
- HY-100456
-
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P1319A
-
|
Nociceptin(1-7) TFA
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
|
-
- HY-13894
-
|
Tyrphostin AG1296
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
|
-
- HY-B0352
-
|
Mirtazapine
Org3770; 6-Azamianserin
|
5-HT Receptor
|
Neurological Disease
|
|
Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
|
-
- HY-13505
-
-
- HY-B0403S
-
|
Bupropion D9
|
Dopamine Receptor
|
Neurological Disease
|
|
Bupropion D9 is a deuterium labeled Bupropion. Bupropion is an atypical antidepressant of the aminoketone group and inhibits dopamine, norepinephrine reuptake and blocks several nicotinic receptors.
|
-
- HY-113962
-
|
7α,25-Dihydroxycholesterol
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
-
- HY-112451
-
-
- HY-13278
-
-
- HY-13736A
-
-
- HY-101756
-
|
SDZ281-977
SDZ-LAP 977
|
Others
|
Cancer
|
|
SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
|
-
- HY-13280
-
-
- HY-112737
-
-
- HY-B0323
-
-
- HY-101310
-
|
SYM 2081
|
iGluR
|
Neurological Disease
|
|
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.
|
-
- HY-133529
-
|
PA-8
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
|
-
- HY-135892
-
|
GNE-1858
|
Others
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
|
-
- HY-15876
-
-
- HY-18840
-
|
BBT594
NVP-BBT594
|
RET
|
Cancer
|
|
BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
|
-
- HY-100154
-
-
- HY-B0310
-
-
- HY-B0004
-
-
- HY-12704
-
-
- HY-B0203A
-
-
- HY-B0203
-
-
- HY-13278A
-
-
- HY-11018
-
-
- HY-B1100
-
-
- HY-15894
-
-
- HY-121450
-
|
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-113756A
-
|
Latanoprost acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
|
-
- HY-N0179
-
|
Ecdysone
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
|
-
- HY-B0128
-
-
- HY-B0381B
-
-
- HY-B0809
-
-
- HY-B0153A
-
-
- HY-19319
-
-
- HY-B0281A
-
-
- HY-B0693
-
-
- HY-10191
-
-
- HY-13955
-
-
- HY-15568A
-
-
- HY-14959
-
|
Ulipristal
CDB-3236; Deacetyl CDB-2914
|
Progesterone Receptor
|
Cancer
Endocrinology
|
|
Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
|
-
- HY-U00002
-
|
ZD-4190
|
VEGFR
EGFR
|
Cancer
|
|
ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
|
-
- HY-15568
-
-
- HY-B0662
-
|
Imidafenacin
KRP-197; ONO-8025
|
mAChR
|
Neurological Disease
|
|
Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).
|
-
- HY-B0106
-
-
- HY-15735
-
|
c-Met inhibitor 1
|
c-Met/HGFR
|
Cancer
|
|
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
|
-
- HY-11018A
-
-
- HY-111255
-
|
SPD304
|
TNF Receptor
|
Cancer
|
|
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
|
-
- HY-114311
-
-
- HY-A0077
-
|
Perphenazine
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-114169
-
|
WRG-28
|
Discoidin Domain Receptor
|
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
|
-
- HY-P1016A
-
-
- HY-103473A
-
|
Boc-MLF TFA
Boc-Met-Leu-Phe-OH (TFA)
|
Others
|
Inflammation/Immunology
|
|
Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
|
-
- HY-110399
-
-
- HY-19816A
-
|
Avitinib maleate
|
EGFR
|
Cancer
|
|
Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM.
|
-
- HY-17005
-
-
- HY-P1250
-
|
RFRP-3(human)
Neuropeptide VF(124-131)(human)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
|
-
- HY-111828
-
|
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-11018B
-
-
- HY-103460
-
|
IRL 2500
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
|
-
- HY-10119
-
|
Vorapaxar
SCH 530348
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-W018931
-
-
- HY-19529
-
-
- HY-P1250A
-
|
RFRP-3(human) TFA
Neuropeptide VF(124-131)(human) TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
RFRP-3 (Neuropeptide VF(124-131))(human) TFA, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
|
-
- HY-12963
-
-
- HY-19748
-
|
LED209
|
Bacterial
|
Infection
|
|
LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
|
-
- HY-100185
-
-
- HY-N0277
-
-
- HY-15252
-
-
- HY-10797
-
|
CJ-42794
CJ-042794
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
CJ-42794 is a selective prostaglandin E receptor subtype 4
(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-13521
-
|
SB-505124
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-P1375
-
|
[D-Trp7,9,10]-Substance P
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-133781
-
|
cis-Clopidogrel-MP Derivative
Clopidogrel-MP-AM
|
Others
|
Others
|
|
cis-Clopidogrel-MP Derivative (Clopidogrel-MP-AM) is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor.
|
-
- HY-14754
-
|
Salirasib
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-100562
-
-
- HY-123205
-
|
Oxatomide
|
Histamine Receptor
P2X Receptor
5-HT Receptor
|
Inflammation/Immunology
|
|
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
|
-
- HY-112322
-
-
- HY-B0478
-
-
- HY-B1895
-
-
- HY-P9902
-
|
Pembrolizumab
MK-3475; Lambrolizumab
|
PD-1/PD-L1
|
Cancer
|
|
Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
|
-
- HY-N0138
-
-
- HY-19969
-
-
- HY-15530
-
-
- HY-10432
-
|
A 83-01
|
ALK
TGF-β Receptor
|
Cancer
|
|
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-135194
-
|
Risperidone E-oxime
|
Others
|
Others
|
|
Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
|
-
- HY-107457
-
|
AZD-8529
|
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-124759
-
-
- HY-12222
-
|
Obeticholic acid
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
|
-
- HY-107457A
-
|
AZD-8529 mesylate
|
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-P1375A
-
|
[D-Trp7,9,10]-Substance P TFA
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-15071
-
|
YM90K
|
iGluR
|
Neurological Disease
|
|
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions.
|
-
- HY-W011400
-
|
TLR1
|
MyD88
|
Inflammation/Immunology
|
|
TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses.
|
-
- HY-P1201
-
|
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-P0118
-
|
Disitertide
P144
|
TGF-beta/Smad
PI3K
|
Cancer
|
Disitertide (P144) is a peptidic TGFβ1 inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor.
|
-
- HY-B0352S
-
|
Mirtazapine D3
Org3770 D3; 6-Azamianserin D3
|
5-HT Receptor
|
Neurological Disease
|
|
Mirtazapine D3 (Org3770 D3; 6-Azamianserin D3) is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
|
-
- HY-14261
-
-
- HY-100739
-
|
RA190
|
Proteasome
|
Cancer
|
|
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
|
-
- HY-B0194A
-
-
- HY-18325
-
-
- HY-B0827
-
|
Dinotefuran
MTI-446
|
Parasite
nAChR
|
Infection
|
|
Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.
|
-
- HY-12075
-
-
- HY-B0194
-
-
- HY-P2273
-
|
Calcitonin (human)
|
CGRP Receptor
|
|
|
Calcitonin human is an endogenous calcitonin receptor agonist.Calcitonin human lowers systemic blood calcium levels and inhibits bone resorption.
|
-
- HY-13226
-
|
Galunisertib
LY2157299
|
TGF-β Receptor
|
Cancer
|
|
Galunisertib (LY2157299) is a oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
|
-
- HY-14149
-
-
- HY-B1305
-
-
- HY-N0686
-
-
- HY-13020
-
-
- HY-B0845
-
|
Prochloraz
BTS 40542
|
Fungal
Estrogen Receptor/ERR
Androgen Receptor
Aryl Hydrocarbon Receptor
|
|
|
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
|
-
- HY-10408
-
|
Ki20227
|
c-Fms
VEGFR
c-Kit
PDGFR
|
Inflammation/Immunology
|
|
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
|
-
- HY-125820
-
-
- HY-108707
-
|
LY3130481
|
iGluR
|
Neurological Disease
|
|
LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC50 of 65 nM.
|
-
- HY-P7061A
-
|
ALX 40-4C Trifluoroacetate
|
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-P7061
-
|
ALX 40-4C
|
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-P0118A
-
|
Disitertide TFA
P144 TFA
|
TGF-beta/Smad
PI3K
|
Cancer
|
Disitertide (P144) TFA is a peptidic TGFβ1 inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor.
|
-
- HY-P0297
-
-
- HY-U00444
-
-
- HY-15283
-
|
Clopidogrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-125567
-
|
Antileukinate
|
CXCR
|
Inflammation/Immunology
|
|
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
|
-
- HY-P1201A
-
|
Cyclosomatostatin TFA
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-17042A
-
|
Cetirizine dihydrochloride
P071
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-17042
-
|
Cetirizine
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-101922
-
-
- HY-B1110
-
|
Nomifensine
(±)-Nomifensin
|
Dopamine Receptor
|
Neurological Disease
|
|
Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
|
-
- HY-A0009
-
-
- HY-P0073
-
-
- HY-100795A
-
-
- HY-100130
-
-
- HY-17390
-
-
- HY-112096
-
|
eCF506
|
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-12043
-
|
SB 525334
|
TGF-β Receptor
|
Cancer
|
|
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
|
-
- HY-101601
-
-
- HY-115496
-
-
- HY-17390A
-
-
- HY-100407
-
|
JNJ16259685
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-136588
-
|
trans-R-138727MP
Prasugrel metabolite R-138727MP
|
P2Y Receptor
|
Cardiovascular Disease
|
|
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-19120
-
|
KB-5492 anhydrous
|
Sigma Receptor
|
Inflammation/Immunology
|
|
KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.
|
-
- HY-A0118A
-
|
Naloxegol oxalate
NKTR-118 oxalate; AZ-13337019 oxalate
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
|
-
- HY-13896
-
|
PD168393
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
|
-
- HY-110249
-
|
CINPA1
|
Others
|
Metabolic Disease
|
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
|
-
- HY-15284
-
|
Prasugrel
PCR 4099
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-N2065
-
|
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-15284A
-
|
Prasugrel hydrochloride
PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-19761
-
-
- HY-32329
-
|
Setiptiline
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-B0545
-
-
- HY-101037
-
|
Sarcosine
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
|
-
- HY-15251
-
-
- HY-101547
-
|
TRPC6-IN-1
|
TRP Channel
|
Cancer
|
|
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
|
-
- HY-B0575
-
-
- HY-13783
-
|
BIBF0775
|
TGF-β Receptor
|
Cancer
|
|
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
|
-
- HY-19900
-
-
- HY-136352
-
|
Adenosine 5'-succinate
|
Others
|
Others
|
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
|
-
- HY-P0090
-
|
Calcitonin (salmon)
Salmon calcitonin
|
CGRP Receptor
|
Cancer
|
|
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
|
-
- HY-B0942
-
-
- HY-16974
-
|
Afoxolaner
|
GABA Receptor
Chloride Channel
|
Infection
|
|
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
|
-
- HY-100660A
-
|
Cetirizine Impurity B dihydrochloride
|
Others
|
Others
|
|
Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
|
-
- HY-129357
-
-
- HY-100661
-
-
- HY-100434
-
|
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-15670
-
|
BMS-906024
|
γ-secretase
Notch
|
Cancer
|
|
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
|
-
- HY-103364A
-
|
C-021 dihydrochloride
|
CCR
|
Inflammation/Immunology
|
|
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [ 35S]GTPγS from binding to the receptor with an IC50 of 18 nM.
|
-
- HY-110028
-
|
Leelamine hydrochloride
|
Cannabinoid Receptor
Fatty Acid Synthase (FASN)
Androgen Receptor
|
Cancer
Endocrinology
|
|
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
|
-
- HY-12987
-
-
- HY-12407
-
|
ZK168281
|
VD/VDR
|
Metabolic Disease
|
|
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
|
-
- HY-103394
-
|
TC HSD 21
|
Others
|
Cancer
|
|
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
|
-
- HY-15494
-
-
- HY-B1473
-
-
- HY-U00200
-
-
- HY-16143
-
|
Cilengitide TFA
EMD 121974 TFA
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
|
-
- HY-13694
-
-
- HY-19189
-
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-15284B
-
|
Prasugrel (Maleic acid)
PCR 4099 (Maleic acid)
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-N0067
-
-
- HY-133555
-
-
- HY-107139
-
|
JNJ-10229570
|
Melanocortin Receptor
|
Endocrinology
|
|
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
|
-
- HY-B0151
-
|
Pregnenolone
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication.
|
-
- HY-P1308
-
-
- HY-P0283
-
-
- HY-131264
-
-
- HY-N1369
-
|
Menthol
|
Others
|
Neurological Disease
|
|
Menthol is a natural analgesic compound. Menthol could cause a feeling of coolness due to stimulation of ‘cold’ receptors by inhibiting Ca ++ currents of neuronal membranes.
|
-
- HY-N0054
-
-
- HY-100506
-
|
GLPG0187
|
Integrin
|
Cancer
|
|
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
|
-
- HY-100013C
-
-
- HY-19205A
-
-
- HY-114349
-
-
- HY-17601
-
-
- HY-108634
-
|
Apafant
WEB 2086
|
Others
|
Inflammation/Immunology
|
|
Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
|
-
- HY-10407
-
|
SU 5402
|
VEGFR
FGFR
PDGFR
|
Cancer
|
|
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
|
-
- HY-13329
-
-
- HY-114492
-
|
GSK547
GSK'547
|
RIP kinase
|
Cancer
|
|
GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
|
-
- HY-B0311A
-
|
Carbidopa monohydrate
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-B0311
-
|
Carbidopa
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-10262
-
-
- HY-15894A
-
|
BQ-788
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
|
-
- HY-105634A
-
|
Nomegestrol acetate
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
|
-
- HY-U00251
-
-
- HY-124957
-
|
α-NETA
|
Apoptosis
|
Cancer
|
|
α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-109139
-
-
- HY-116564
-
|
Lotilaner
|
Parasite
GABA Receptor
|
Infection
|
|
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.
|
-
- HY-P1308A
-
-
- HY-17042AS
-
|
Cetirizine D4 dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cetirizine D4 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-17042S
-
|
Cetirizine D4
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-17042S1
-
|
Cetirizine D8
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-17042AS1
-
|
Cetirizine D8 dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cetirizine D8 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-N0170
-
-
- HY-10431
-
-
- HY-19960
-
|
BCTC
|
TRP Channel
|
Cancer
|
|
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
|
-
- HY-101238
-
-
- HY-12806
-
|
AG1557
|
EGFR
|
Cancer
|
|
AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
|
-
- HY-13277
-
-
- HY-P1514
-
-
- HY-P0201
-
-
- HY-133533
-
|
O-2050
|
Cannabinoid Receptor
|
|
|
O-2050 is a high affinity cannabinoid CB1 receptor silent antagonist. O-2050 also acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC50=40.4 nM). O-2050 antagonizes effects of CP-55940 in vitro.
|
-
- HY-N1881
-
|
4',5-Dihydroxyflavone
|
Lipoxygenase
Glucosidase
|
Others
|
|
4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
|
-
- HY-14234
-
-
- HY-50175
-
-
- HY-P1209A
-
-
- HY-109010
-
|
Poseltinib
HM71224; LY3337641
|
Btk
BMX Kinase
Toll-like Receptor (TLR)
|
Metabolic Disease
|
|
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
|
-
- HY-B0135A
-
|
Furosemide sodium
|
NKCC
|
Cancer
Metabolic Disease
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-B0135
-
|
Furosemide
|
NKCC
|
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-B1739
-
|
Pregnenolone monosulfate
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication.
|
-
- HY-110189
-
|
Pregnenolone monosulfate sodium salt
3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
|
-
- HY-135590
-
-
- HY-13016
-
-
- HY-135584
-
|
Raloxifene 6-Monomethyl Ether
|
Estrogen Receptor/ERR
|
|
|
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.
|
-
- HY-P1209
-
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-101583
-
-
- HY-114392
-
|
Gly-β-MCA
|
FXR
Autophagy
|
Metabolic Disease
|
|
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
|
-
- HY-B1789A
-
-
- HY-107782
-
-
- HY-108522
-
|
PA452
|
RAR/RXR
|
Metabolic Disease
|
|
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
|
-
- HY-18785
-
-
- HY-135811
-
-
- HY-120081A
-
|
Metixene hydrochloride hydrate
|
mAChR
|
Neurological Disease
|
|
Metixene hydrochloride hydrate is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM.
|
-
- HY-116514
-
-
- HY-N2337
-
-
- HY-10501
-
|
SU14813
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
|
-
- HY-120081B
-
|
Metixene hydrochloride
|
mAChR
|
Neurological Disease
|
|
Metixene hydrochloride is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM.
|
-
- HY-10501A
-
-
- HY-108465
-
|
Pyr3
|
TRP Channel
|
Others
|
|
Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
|
-
- HY-B0548
-
-
- HY-B0548A
-
-
- HY-15539
-
-
- HY-A0007
-
-
- HY-B2158
-
-
- HY-114492A
-
|
(Rac)-GSK547
|
RIP kinase
|
Cancer
|
|
(Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
|
-
- HY-W031727
-
-
- HY-103355
-
|
YM022
|
CCR
|
Metabolic Disease
|
|
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
|
-
- HY-12143
-
-
- HY-15086
-
|
Selfotel
CGS 19755
|
iGluR
|
Neurological Disease
|
|
Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM.
|
-
- HY-15023
-
|
Cligosiban
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-100113
-
-
- HY-B0895
-
-
- HY-P1481
-
-
- HY-P0216
-
-
- HY-100366
-
-
- HY-N0060
-
-
- HY-P9905
-
|
Cetuximab
C225
|
EGFR
|
Cancer
|
|
Cetuximab (C225) is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for soluble EGFR by SPR. Cetuximab has potent antitumor activity.
|
-
- HY-B1388
-
|
Homatropine methylbromide
Homatropine methobromide
|
mAChR
|
Neurological Disease
|
|
Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
|
-
- HY-N0060A
-
-
- HY-78349
-
|
A 77-01
|
TGF-β Receptor
|
Cancer
|
|
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
|
-
- HY-12684
-
|
CH-223191
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR).
CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
|
-
- HY-B0725
-
-
- HY-122575
-
|
Aurintricarboxylic acid
|
P2X Receptor
Influenza Virus
Topoisomerase
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM.
|
-
- HY-15394
-
-
- HY-P1106
-
|
K41498
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study.
|
-
- HY-P0201A
-
-
- HY-13274
-
-
- HY-50159
-
-
- HY-50158
-
-
- HY-14649
-
|
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-129995
-
|
TSHR antagonist S37b
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37b is an enantiomer of TSHR antagonist S37a (HY-129995A), shows only a minor effect for TSHR inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
|
-
- HY-P2307
-
|
Tat-NR2Baa
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-P2307A
-
|
Tat-NR2Baa TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-104021
-
|
GSK840
GSK'840
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
|
-
- HY-10794
-
-
- HY-16141
-
|
Cilengitide
EMD 121974
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide, a cyclic RGD-containing peptide, is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.
|
-
- HY-128878
-
-
- HY-18719B
-
-
- HY-12423A
-
|
TAS-115 mesylate
TAS-115 methanesulfonate
|
VEGFR
c-Met/HGFR
|
Cancer
|
|
TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
|
-
- HY-12423
-
|
TAS-115
|
VEGFR
c-Met/HGFR
|
Cancer
|
|
TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
|
-
- HY-135811A
-
-
- HY-15484
-
-
- HY-103306
-
|
Ryanodine
|
Others
|
Neurological Disease
|
|
Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
|
-
- HY-18719E
-
-
- HY-101038A
-
-
- HY-102093
-
-
- HY-19250
-
-
- HY-N2371
-
-
- HY-U00339
-
-
- HY-50713
-
-
- HY-P1276A
-
-
- HY-18347A
-
-
- HY-14218
-
-
- HY-10418
-
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- HY-120179A
-
|
LP-922761 hydrate
|
Others
|
Neurological Disease
|
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-120179
-
|
LP-922761
|
Others
|
Neurological Disease
|
|
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-18990
-
|
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-125402
-
|
GSK-843
GSK'843
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
|
-
- HY-14127
-
|
R121919
NBI30775
|
CRFR
|
Neurological Disease
Endocrinology
|
|
R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
|
-
- HY-101308A
-
|
MRS2179 tetrasodium hydrate
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.
|
-
- HY-107723
-
-
- HY-14567
-
-
- HY-15498
-
|
Rimegepant
BMS-927711
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
|
-
- HY-128585
-
-
- HY-15043
-
-
- HY-100183
-
-
- HY-B0365A
-
-
- HY-12823
-
|
BLU9931
|
FGFR
|
Cancer
|
|
BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity.
|
-
- HY-100691
-
-
- HY-10013
-
|
Taranabant
MK-0364
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
|
-
- HY-N0737
-
-
- HY-133781S
-
|
cis-Clopidogrel-MP Derivative 13CD3
Clopidogrel-MP-AM 13CD3
|
Others
|
Others
|
|
cis-Clopidogrel-MP Derivative 13CD3 (Clopidogrel-MP-AM 13CD3) is a deuterium labele cis-Clopidogrel-MP Derivative. cis-Clopidogrel-MP Derivative is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor.
|
-
- HY-N7652
-
|
Terminolic acid
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity.
|
-
- HY-103104
-
|
Fananserin
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-12749
-
-
- HY-13101
-
-
- HY-103533
-
-
- HY-P2546
-
|
Biotin-Substance P
|
Neurokinin Receptor
|
Neurological Disease
|
|
Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
|
-
- HY-B1370A
-
-
- HY-112847A
-
|
Sulfosuccinimidyl oleate sodium
Sulfo-N-succinimidyl oleate sodium
|
Mitophagy
|
Inflammation/Immunology
|
|
Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
|
-
- HY-15897
-
|
LDN-212854
|
TGF-β Receptor
|
Cancer
|
|
LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
|
-
- HY-12044
-
|
Cabozantinib S-malate
XL184 S-malate; BMS-907351 S-malate
|
VEGFR
Apoptosis
|
Cancer
|
|
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-B1370
-
-
- HY-103021
-
|
LY3200882
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
|
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
|
-
- HY-112847
-
|
Sulfosuccinimidyl oleate
Sulfo-N-succinimidyl oleate
|
Mitophagy
|
Inflammation/Immunology
|
|
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
|
-
- HY-102024
-
-
- HY-15289
-
-
- HY-101232
-
|
Tiotidine
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
|
-
- HY-14335
-
|
Ro 04-6790
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors.
|
-
- HY-P1840
-
-
- HY-112558
-
-
- HY-12749A
-
-
- HY-U00253
-
-
- HY-B0366A
-
-
- HY-B0406
-
|
Bethanechol
Carbamyl-β-methylcholine
|
mAChR
|
Neurological Disease
|
|
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.
|
-
- HY-B0406A
-
|
Bethanechol chloride
Carbamyl-β-methylcholine chloride
|
mAChR
|
Metabolic Disease
|
|
Bethanechol Chloride (Carbamyl-β-methylcholine chloride) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.
|
-
- HY-B0412
-
-
- HY-B0469
-
-
- HY-16734A
-
|
Amiselimod hydrochloride
MT-1303 hydrochloride
|
LPL Receptor
|
Cancer
|
|
Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
|
-
- HY-105272A
-
-
- HY-B1270
-
-
- HY-105272
-
|
Loreclezole
R 72063
|
GABA Receptor
|
Neurological Disease
|
|
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
|
-
- HY-101626
-
-
- HY-10309
-
|
Sibrafiban
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
|
-
- HY-13613
-
|
Dutasteride
GG 745; GI 198745
|
5 alpha Reductase
Apoptosis
|
Cancer
|
|
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
|
-
- HY-107500
-
|
UVI 3003
|
RAR/RXR
Autophagy
|
Others
|
|
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
|
-
- HY-B0418A
-
-
- HY-16446
-
|
SAR125844
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays.
|
-
- HY-12071
-
|
LDN193189
DM-3189
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
|
-
- HY-50867
-
|
Lestaurtinib
CEP-701; KT-5555
|
JAK
FLT3
Trk Receptor
|
Cancer
|
|
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
|
-
- HY-B0144A
-
-
- HY-B1370B
-
-
- HY-131262
-
|
Hydroxychloroquine Impurity E
4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol
|
Others
|
Others
|
|
Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
|
-
- HY-121300
-
|
Kendomycin
(-)-TAN2162
|
Antibiotic
Bacterial
Endothelin Receptor
CGRP Receptor
|
Cancer
Infection
|
|
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
|
-
- HY-10656
-
|
SB-657510
|
Urotensin Receptor
|
Inflammation/Immunology
|
|
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.
|
-
- HY-15039
-
|
SSR240612
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-108400
-
|
SCH-23390 maleate
R-(+)-SCH-23390 maleate
|
Dopamine Receptor
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
|
-
- HY-19545A
-
|
SCH-23390 hydrochloride
R-(+)-SCH-23390 hydrochloride
|
Dopamine Receptor
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
|
-
- HY-106660
-
|
BP 897
|
Dopamine Receptor
|
Neurological Disease
|
|
BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 µM, respectively).
|
-
- HY-101641
-
-
- HY-116637
-
|
Tetrahydromagnolol
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
|
-
- HY-P1840A
-
-
- HY-16751
-
-
- HY-107982
-
|
VU6005649
|
mGluR
|
Neurological Disease
|
|
VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
|
-
- HY-P1758
-
-
- HY-101704
-
-
- HY-17512
-
-
- HY-15195
-
-
- HY-14870
-
-
- HY-10634
-
-
- HY-133486
-
-
- HY-19308
-
-
- HY-15541
-
-
- HY-17551
-
-
- HY-12882A
-
|
Ifenprodil tartrate
|
iGluR
Potassium Channel
|
Neurological Disease
|
|
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.
|
-
- HY-136587
-
|
Oxomemazine
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment.
|
-
- HY-12071A
-
|
LDN193189 Tetrahydrochloride
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
|
-
- HY-B0725S
-
|
Doxepin D3 Hydrochloride
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
|
|
Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
|
-
- HY-130254
-
|
Src Inhibitor 3
|
Src
|
Cancer
Inflammation/Immunology
|
|
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
|
-
- HY-12866
-
|
Larotrectinib
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-120142
-
|
EC359
|
Apoptosis
|
Cancer
|
|
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.
|
-
- HY-112815
-
|
ALK2-IN-2
|
TGF-β Receptor
|
Cancer
|
|
ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
|
-
- HY-N7512
-
|
Asimilobine
|
Dopamine Receptor
5-HT Receptor
Parasite
|
Cancer
Infection
|
|
Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
|
-
- HY-30234
-
-
- HY-119093
-
-
- HY-13979
-
-
- HY-N4095
-
-
- HY-30234A
-
-
- HY-15771A
-
|
Tirabrutinib hydrochloride
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
|
Cancer
|
|
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
|
-
- HY-W010841
-
|
Levocetirizine dihydrochloride
(R)-Cetirizine dihydrochloride
|
Histamine Receptor
|
Endocrinology
Inflammation/Immunology
|
|
Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
|
-
- HY-B0814
-
|
Levocetirizine
(R)-Cetirizine
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
|
-
- HY-113008A
-
|
cis-Urocanic acid
(Z)-Urocanic acid; cis-UCA
|
5-HT Receptor
|
Inflammation/Immunology
|
|
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
|
-
- HY-14539
-
|
Clozapine
HF 1854
|
Dopamine Receptor
mAChR
|
Neurological Disease
|
|
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
|
-
- HY-12987S
-
-
- HY-122537A
-
|
Arotinolol
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
|
-
- HY-19945
-
|
DAA-1106
|
GABA Receptor
|
Neurological Disease
|
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
- HY-12111
-
-
- HY-114025
-
-
- HY-B0726
-
-
- HY-10486
-
-
- HY-10088
-
-
- HY-P1536
-
-
- HY-118557
-
|
Iferanserin
S-MPEC
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment.
|
-
- HY-B1281
-
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-111767
-
|
BAY-545
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
|
-
- HY-136427
-
|
KRM-III
|
Others
|
Inflammation/Immunology
|
|
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
|
-
- HY-14134
-
|
BMS-378806
BMS-806
|
HIV
|
Infection
|
|
BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.
|
-
- HY-19733
-
-
- HY-108912
-
-
- HY-W011955
-
-
- HY-12290
-
|
Arg-Gly-Asp-Ser
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
|
-
- HY-10517
-
|
Orantinib
SU6668; TSU-68
|
PDGFR
FGFR
VEGFR
Apoptosis
|
Cancer
|
|
Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
|
-
- HY-P0224
-
-
- HY-14136
-
-
- HY-P0318
-
-
- HY-103178
-
|
MRE3008F20
|
Adenosine Receptor
|
Cancer
|
|
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
|
-
- HY-14137
-
-
- HY-10792A
-
-
- HY-112823B
-
|
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
|
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
|
-
- HY-N0250
-
-
- HY-B1813A
-
|
(±)-Vesamicol hydrochloride
(±)-AH5183 hydrochloride
|
Sigma Receptor
|
Neurological Disease
|
|
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.
|
-
- HY-B1006
-
-
- HY-101420
-
-
- HY-P1467
-
-
- HY-U00077
-
-
- HY-19048
-
-
- HY-113356
-
-
- HY-B0548S1
-
-
- HY-U00360
-
-
- HY-110193
-
|
SPP-86
|
RET
|
Cancer
|
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
|
-
- HY-109095
-
-
- HY-15445
-
|
CTEP
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.
|
-
- HY-B1794A
-
-
- HY-100008
-
|
Peretinoin
NIK333
|
RAR/RXR
SPHK
Autophagy
HCV
|
Cancer
Infection
|
|
Peretinoin is an oral acyclic retinoid retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
|
-
- HY-106994A
-
|
Nebentan potassium
YM598
|
Endothelin Receptor
|
Inflammation/Immunology
|
|
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
|
-
- HY-12076
-
|
BMS 777607
BMS 817378
|
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
|
-
- HY-P1467A
-
-
- HY-15618
-
-
- HY-15538
-
-
- HY-70050C
-
-
- HY-70050A
-
-
- HY-12940
-
-
- HY-P1588
-
-
- HY-121877
-
|
Valnoctamide
Valmethamide
|
GABA Receptor
|
Neurological Disease
|
|
Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors.
|
-
- HY-10900
-
-
- HY-13788
-
-
- HY-Y1683
-
|
DL-Menthol
Racementhol
|
GABA Receptor
|
Others
|
|
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol induces surgical anesthesia for fish that relates to the activation of GABAA receptor.
|
-
- HY-100856
-
-
- HY-U00429
-
-
- HY-111444
-
|
Auxinole
|
Others
|
Others
|
|
Auxinole is a potent auxin antagonist of TIR1/AFB receptors, binding TIR1 to block the formation of the TIR1-IAA-Aux/IAA complex and so inhibits auxin-responsive gene expression.
|
-
- HY-107790
-
|
5-Methoxyflavone
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
|
-
- HY-13223
-
|
Crenolanib
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-103017
-
|
JH-X-119-01 hydrochloride
|
IRAK
|
Infection
|
|
JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.
|
-
- HY-N0020
-
|
Echinacoside
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
|
-
- HY-101032
-
|
RIPA-56
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting
protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome.
|
-
- HY-117508
-
-
- HY-B1693
-
|
Levomepromazine
Methotrimeprazine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Levomepromazine (Methotrimeprazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors.
|
-
- HY-100301
-
-
- HY-P1502
-
|
β-Endorphin, human
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
|
-
- HY-P2510
-
-
- HY-16661
-
|
Skp2 Inhibitor C1
SKPin C1
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
|
-
- HY-N2345
-
|
Procyanidin B3
|
Histone Acetyltransferase
|
Cancer
|
|
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
|
-
- HY-101333
-
|
CPPG
(RS)-CPPG
|
mGluR
|
Neurological Disease
|
|
CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
|
-
- HY-111455
-
|
LP-211
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-125819
-
-
- HY-10061
-
|
Lesogaberan
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.
|
-
- HY-110201
-
|
Estrogen receptor modulator 1
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
|
-
- HY-B0020
-
-
- HY-106993
-
|
Cipralisant
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has the potential for attention-deficit hyperactivity disorder treatment.
|
-
- HY-U00420
-
-
- HY-19365
-
-
- HY-17571
-
|
Oxytocin
α-Hypophamine; Oxytocic hormone
|
Oxytocin Receptor
|
Endocrinology
|
|
Oxytocin (α-Hypophamine) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
|
-
- HY-17428
-
-
- HY-128975
-
-
- HY-15540
-
-
- HY-15653
-
-
- HY-13338S
-
-
- HY-12127
-
-
- HY-17571A
-
|
Oxytocin acetate
α-Hypophamine acetate; Oxytocic hormone acetate
|
Oxytocin Receptor
|
Endocrinology
|
|
Oxytocin acetate (α-Hypophamine acetate) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
|
-
- HY-17351
-
-
- HY-112679
-
-
- HY-106994
-
|
Nebentan
YM598 free base
|
Endothelin Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
|
-
- HY-10524
-
|
GSK1904529A
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
|
-
- HY-N0737A
-
|
Harmine
Telepathine
|
DYRK
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
|
-
- HY-P1537
-
-
- HY-114412A
-
-
- HY-14406A
-
-
- HY-14609
-
|
MPEP Hydrochloride
|
mGluR
|
Neurological Disease
|
|
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects.
|
-
- HY-14609A
-
|
MPEP
|
mGluR
|
Neurological Disease
|
|
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects.
|
-
- HY-P1107
-
|
Antisauvagine-30
aSvg-30
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively.
|
-
- HY-16963
-
-
- HY-110000
-
-
- HY-107563A
-
|
ROS 234 dioxalate
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
|
-
- HY-B0623A
-
|
Ropinirole hydrochloride
SKF 101468 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
|
-
- HY-103241
-
|
Ro 90-7501
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
|
-
- HY-B1505
-
-
- HY-N1427A
-
-
- HY-100248
-
-
- HY-B1532
-
-
- HY-B1833
-
-
- HY-32329A
-
-
- HY-100810
-
-
- HY-14994
-
|
SCH79797 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-119687
-
|
Bifenazate
|
GABA Receptor
|
Infection
|
|
Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor.
|
-
- HY-P0298
-
-
- HY-14782
-
-
- HY-12509
-
|
PEPA
|
iGluR
|
Neurological Disease
|
|
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
|
-
- HY-P1276
-
-
- HY-P9903
-
|
Nivolumab
BMS-936558; ONO-4538; MDX-1106
|
PD-1/PD-L1
|
Cancer
|
|
Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody to treat advanced (metastatic) non-small cell lung cancer.
|
-
- HY-P0298A
-
-
- HY-15370
-
-
- HY-B0469S
-
-
- HY-N1166
-
|
Tephrosin
Deguelinol I; Hydroxydeguelin
|
EGFR
|
Cancer
|
|
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
|
-
- HY-10021
-
-
- HY-B0377
-
-
- HY-U00238
-
-
- HY-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- HY-B0072
-
-
- HY-103286
-
|
PD176252
|
Bombesin Receptor
|
Cancer
|
|
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
|
-
- HY-129390
-
|
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-19928A
-
|
Vactosertib Hydrochloride
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.
|
-
- HY-10330
-
|
Toceranib
SU11654; PHA 291639E
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
|
-
- HY-135671
-
-
- HY-118482
-
|
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-109091
-
|
Lanraplenib
GS-9876
|
Syk
|
Inflammation/Immunology
|
|
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
|
-
- HY-10330A
-
|
Toceranib phosphate
SU11654 phosphate; PHA 291639E phosphate
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
|
-
- HY-19928
-
|
Vactosertib
EW-7197; TEW-7197
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.
|
-
- HY-111372
-
|
Finerenone
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
|
-
- HY-14873
-
|
Tonapofylline
BG 9928
|
Adenosine Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
|
-
- HY-136142
-
|
Prasugrel chloride impurity
|
Others
|
Others
|
|
Prasugrel chloride impurity is a catp impurity of Prasugrel, exacted from patent US20130345428A1, line 0053. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-119039
-
|
RU-301
|
TAM Receptor
|
Cancer
|
|
RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively.
|
-
- HY-N2510
-
|
Myristicin
Myristicine
|
5-HT Receptor
|
Neurological Disease
|
|
Myristicine act as a serotonin receptor antagonist, a weak monamine oxidase (MAO) inhibitor. Myristicine is the main component of nutmeg essential oil from Myristica fragrans Houtt. Myristicine abuse produce hallucinogenic effects, organ damage, deliriumand others.
|
-
- HY-N7045
-
|
Isosilybin B
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
|
-
- HY-102004
-
-
- HY-136299
-
|
Sepimostat
FUT-187 free base
|
iGluR
|
Neurological Disease
|
|
Sepimostat exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
|
-
- HY-12501
-
|
ITI214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
|
-
- HY-B0285
-
-
- HY-B0285A
-
-
- HY-N0499
-
|
Cyanidin Chloride
IdB 1027
|
Others
|
Cancer
|
|
Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression.
|
-
- HY-B0640A
-
-
- HY-133024
-
|
Flumexadol
|
5-HT Receptor
|
Neurological Disease
|
|
Flumexadol is an orally active non-narcotic analgesic. Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor.
|
-
- HY-135581
-
|
Raloxifene 6-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-100943
-
|
Cinanserin hydrochloride
SQ 10643
|
5-HT Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
|
-
- HY-119706
-
|
Barbadin
|
Others
|
Others
|
|
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.
|
-
- HY-103565
-
|
AMN082
|
mGluR
|
Neurological Disease
|
|
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
|
-
- HY-135582
-
|
Raloxifene 4'-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-B0031S
-
-
- HY-111669
-
-
- HY-13044
-
-
- HY-13604
-
-
- HY-U00185
-
-
- HY-112185
-
-
- HY-P1462
-
-
- HY-101619
-
-
- HY-P1481A
-
-
- HY-10633
-
-
- HY-129029
-
|
Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-11030A
-
-
- HY-101980
-
|
AZD4635
htL1071
|
Adenosine Receptor
|
Cancer
|
|
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
|
-
- HY-125821
-
|
Sigma-1 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
|
-
- HY-10171
-
|
NPS-2143 hydrochloride
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-10007
-
|
NPS-2143
SB-262470A
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-14544
-
|
Quetiapine
ICI204636
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
|
-
- HY-B0031
-
|
Quetiapine hemifumarate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
|
-
- HY-N4121
-
|
Isocurcumenol
|
Estrogen Receptor/ERR
Apoptosis
|
|
|
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
|
-
- HY-N2600
-
|
Kuwanon H
|
Bombesin Receptor
|
Cancer
|
|
Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
|
-
- HY-19764
-
|
GSK2983559 active metabolite
|
RIP kinase
|
Cancer
|
|
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
|
-
- HY-B0640
-
-
- HY-N2078
-
|
Yamogenin
Neodiosgenin
|
LXR
|
Metabolic Disease
|
|
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
|
-
- HY-100461
-
-
- HY-16991
-
-
- HY-42068
-
-
- HY-B1547A
-
-
- HY-100280
-
-
- HY-100266
-
-
- HY-B1829A
-
-
- HY-B1392
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-U00281
-
-
- HY-U00227
-
-
- HY-15122
-
-
- HY-I0230
-
-
- HY-12870A
-
|
AZD9496 maleate
|
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-P1462A
-
-
- HY-B0164A
-
-
- HY-112189
-
-
- HY-10889
-
-
- HY-B0164
-
-
- HY-107384
-
-
- HY-U00104
-
|
YM-46303
|
mAChR
|
Endocrinology
|
|
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
|
-
- HY-13683
-
-
- HY-12142
-
-
- HY-12761
-
-
- HY-12870
-
|
AZD9496
|
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-15419
-
|
RS-127445 hydrochloride
|
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-B0436
-
-
- HY-19533
-
|
SCH 58261
|
Adenosine Receptor
|
Cancer
|
|
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
|
-
- HY-B0781
-
-
- HY-15419A
-
|
RS-127445
|
5-HT Receptor
|
Neurological Disease
|
|
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-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-116767
-
|
BLT-1
|
HCV
|
Metabolic Disease
Inflammation/Immunology
|
|
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor. BLT-1 has pro-inflammatory functions through neutrophil recruitment.
|
-
- HY-11109
-
-
- HY-114181
-
|
IRAK4-IN-4
|
IRAK
|
Inflammation/Immunology
|
|
IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
|
-
- HY-18204A
-
|
LCZ696
Sacubitril/Valsartan
|
Angiotensin Receptor
Neprilysin
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
LCZ696 (Sacubitril/Valsartan), comprised Valsartan (an ARB) 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. LCZ696 ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.
|
-
- HY-P1119
-
|
WRW4
|
Others
|
Neurological Disease
|
|
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
|
-
- HY-14674
-
|
CP-724714
|
EGFR
Apoptosis
|
Cancer
|
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
|
-
- HY-106199
-
-
- HY-P1316
-
|
Ac-RYYRWK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-P1316A
-
|
Ac-RYYRWK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-13222
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-12705A
-
-
- HY-15418
-
-
- HY-129946
-
-
- HY-15122A
-
-
- HY-B0524A
-
-
- HY-B1052
-
-
- HY-14339
-
-
- HY-104003
-
-
- HY-B1052A
-
-
- HY-10871
-
-
- HY-D0237
-
-
- HY-B0524
-
-
- HY-11029
-
-
- HY-19947
-
|
PF-06291874
Glucagon receptor antagonists-4
|
Glucagon Receptor
|
Metabolic Disease
|
|
PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs.
|
-
- HY-B0005A
-
|
Toremifene
Z-Toremifene; NK 622 free base; FC-1157a free base
|
Estrogen Receptor/ERR
|
Cancer
Infection
|
|
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-12768
-
|
BLZ945
|
c-Fms
|
Cancer
|
|
BLZ945 is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
|
-
- HY-N1943
-
-
- HY-121356
-
|
Carebastine
|
Histamine Receptor
|
Cancer
Endocrinology
|
|
Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
|
-
- HY-U00064
-
|
AZD2098
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
AZD2098 is a potent and selective CC-chemokine receptor 4 (CCR4) inhibitor with pIC50s of 7.8, 8.0, 8.0 and 7.6 for human, rat, mouse and dog respectively, used for asthma research.
|
-
- HY-18991
-
|
CCG215022
|
PKA
|
Cancer
|
|
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
|
-
- HY-10799
-
|
EG00229
|
Complement System
|
Cancer
|
|
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.
|
-
- HY-12866A
-
|
Larotrectinib sulfate
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-119744
-
|
BAY 38-7271
|
Cannabinoid Receptor
|
Neurological Disease
|
|
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
|
-
- HY-136281
-
|
DuP 734
|
Sigma Receptor
|
Neurological Disease
|
|
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.
|
-
- HY-107743
-
|
Naloxone benzoylhydrazone
NalBzoH
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.
|
-
- HY-100703
-
-
- HY-101630
-
|
Deramciclane
EGIS-3886
|
5-HT Receptor
|
Neurological Disease
|
|
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
|
-
- HY-16978
-
-
- HY-101265
-
|
S1p receptor agonist 1
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.
|
-
- HY-105685
-
|
SRX246
|
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-103152
-
-
- HY-13242
-
|
Taladegib
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
-
- HY-10053
-
-
- HY-113413
-
-
- HY-B1540
-
-
- HY-106910
-
-
- HY-12525
-
-
- HY-B0461
-
-
- HY-P1000
-
-
- HY-B1589A
-
-
- HY-101574
-
-
- HY-U00062
-
-
- HY-U00016
-
-
- HY-19065
-
-
- HY-B1240
-
-
- HY-P0187
-
-
- HY-B0480
-
-
- HY-B0664
-
-
- HY-13291
-
-
- HY-B0031S1
-
-
- HY-13527
-
-
- HY-14121
-
-
- HY-U00321
-
-
- HY-32709
-
|
Telcagepant
MK-0974
|
CGRP Receptor
|
Neurological Disease
|
|
Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
|
-
- HY-108463
-
|
A-967079
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-A0002
-
-
- HY-N2338
-
-
- HY-B0548S
-
-
- HY-P1083
-
-
- HY-19381
-
-
- HY-16579A
-
|
Etifoxine
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors.
|
-
- HY-P1766
-
-
- HY-B0548AS
-
-
- HY-P1548
-
-
- HY-P1548B
-
-
- HY-14813
-
|
Cutamesine
SA4503; AGY 94806
|
Sigma Receptor
|
Neurological Disease
|
|
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
|
-
- HY-101588
-
|
Gefapixant
MK-7264; AF-219
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant (MK-7264) is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
|
-
- HY-103414
-
|
Raclopride
|
Dopamine Receptor
|
Neurological Disease
|
|
Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively.
|
-
- HY-15010
-
|
L-371,257
|
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-107642
-
|
MA-2029
|
Motilin Receptor
|
Metabolic Disease
|
|
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility.
|
-
- HY-10791
-
-
- HY-107691
-
|
GR 159897
|
Neurokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
|
-
- HY-P1066
-
|
Apelin-17(human, bovine)
|
HIV
|
Infection
|
|
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-P1065
-
|
Apelin-36(rat, mouse)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-109091B
-
|
Lanraplenib succinate
GS-9876 succinate
|
Syk
|
Inflammation/Immunology
|
|
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
|
-
- HY-100131
-
|
GSK481
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
|
-
- HY-13203
-
-
- HY-15185
-
|
Nirogacestat
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-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-N4053
-
|
Heraclenin
|
Others
|
Inflammation/Immunology
|
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-B0285B
-
-
- HY-P1271
-
|
Catestatin
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-P1333
-
|
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-50697
-
-
- HY-P0272
-
|
Peptide T
|
HIV
|
Infection
|
|
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-17043
-
-
- HY-105542
-
-
- HY-105634
-
|
Nomegestrol
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-U00180
-
-
- HY-100815B
-
|
(RS)-AMPA
(±)-AMPA
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors.
|
-
- HY-A0034
-
|
Solifenacin
YM905 free base
|
mAChR
|
Neurological Disease
|
|
Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-70068
-
-
- HY-14825A
-
-
- HY-10806
-
-
- HY-P1866
-
-
- HY-14151
-
|
Prucalopride
|
5-HT Receptor
|
Neurological Disease
|
|
Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.
|
-
- HY-13104
-
-
- HY-P1548A
-
-
- HY-14539S
-
|
Clozapine D8
HF 1854 D8
|
Dopamine Receptor
mAChR
|
Neurological Disease
|
|
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-10432A
-
|
A 83-01 sodium salt
|
TGF-β Receptor
ALK
|
Cancer
|
|
A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-101529
-
|
Imanixil
HOE-402(free base)
|
Others
|
Cardiovascular Disease
|
|
Imanixil (HOE-402 free base) is an inducer of the LDL receptor (LDLR). Imanixil (HOE-402 free base) is also a potent cholesterol-lowering compound, which inhibits very low density-lipoprotein (VLDL) production, and consequently attenuates atherosclerosis development.
|
-
- HY-P9926
-
-
- HY-101483
-
|
Dihydromunduletone
DHM
|
Others
|
Cancer
Neurological Disease
|
|
Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
|
-
- HY-121685A
-
|
Tipepidine hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
|
-
- HY-13636
-
|
Fulvestrant
ICI 182780; ZD 9238; ZM 182780
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
|
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
|
-
- HY-N0366
-
|
Sennoside B
|
PDGFR
|
Cancer
|
|
Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
|
-
- HY-P1293
-
|
Conantokin G
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
|
-
- HY-101534
-
-
- HY-B0661
-
-
- HY-U00315
-
-
- HY-U00245
-
-
- HY-U00205
-
-
- HY-U00202
-
-
- HY-B0561
-
-
- HY-B0460
-
-
- HY-100173
-
-
- HY-100903
-
-
- HY-N0219
-
-
- HY-U00110
-
-
- HY-103531
-
-
- HY-10473
-
-
- HY-U00123
-
-
- HY-P0262
-
-
- HY-101691
-
-
- HY-100785
-
-
- HY-A0173
-
-
- HY-B1303A
-
-
- HY-13209
-
-
- HY-17416A
-
-
- HY-A0129
-
-
- HY-N1415
-
-
- HY-B2154
-
-
- HY-N2096
-
|
Kavain
|
GABA Receptor
|
Neurological Disease
|
|
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
|
-
- HY-107051
-
-
- HY-101690
-
-
- HY-N4157
-
-
- HY-10805A
-
-
- HY-G0014B
-
-
- HY-N2310
-
|
Domoic acid
(-)-Domoic acid; L-Domoic acid
|
iGluR
|
Neurological Disease
|
|
Domoic acid ((-)-Domoic acid; L-Domoic acid) is an excitatory neurotransmitter isolated from a form of marine vegetation, Nitzschia pungens. Domoic acid produces neurotoxic effect through activating kainate receptor.
|
-
- HY-G0014A
-
-
- HY-P0272A
-
|
Peptide T TFA
|
HIV
|
Infection
|
|
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-100155
-
|
4-IBP
|
Sigma Receptor
|
Cancer
|
|
4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
|
-
- HY-17512S
-
-
- HY-10898
-
-
- HY-10805
-
-
- HY-P1866A
-
-
- HY-P1083A
-
-
- HY-15072
-
|
Zonampanel
YM 872
|
iGluR
|
Metabolic Disease
|
|
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
|
-
- HY-19574
-
-
- HY-12641
-
|
Pyrantel tartrate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.
|
-
- HY-10252
-
|
NVP-ADW742
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
|
-
- HY-B0144
-
|
Pitavastatin Calcium
NK-104 hemicalcium; Pitavastatin hemicalcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Mitophagy
Apoptosis
|
Metabolic Disease
Cancer
|
|
Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
|
-
- HY-14422
-
|
SR1078
|
ROR
|
Cancer
|
|
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
|
-
- HY-130992
-
-
- HY-14940
-
|
Volinanserin
MDL100907; M 100907
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
|
-
- HY-N0175
-
|
Cytisinicline
Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
|
|
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
|
-
- HY-13706
-
|
CAY10471 Racemate
TM30089 Racemate
|
Prostaglandin Receptor
|
Cancer
Endocrinology
|
|
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2.
|
-
- HY-103430
-
|
SKF-83566 hydrobromide
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
|
-
- HY-P1110
-
|
AF12198
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
|
-
- HY-103430A
-
|
SKF-83566
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
|
-
- HY-U00367
-
-
- HY-P1333A
-
|
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-101385
-
-
- HY-13713
-
-
- HY-P1019A
-
-
- HY-124543
-
-
- HY-103546
-
-
- HY-N0908
-
-
- HY-14590
-
-
- HY-P1401
-
|
Protein Kinase C (19-36)
|
PKC
|
Metabolic Disease
|
|
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response.
|
-
- HY-100492
-
|
Fisogatinib
BLU-554
|
FGFR
|
Cancer
|
|
Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.
|
-
- HY-10331
-
|
Regorafenib
BAY 73-4506
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
|
-
- HY-B0005
-
|
Toremifene citrate
Z-Toremifene citrate; NK 622; FC-1157a
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Infection
|
|
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-13290
-
|
KN-62
|
CaMK
P2X Receptor
Autophagy
|
Metabolic Disease
Cancer
|
|
KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-11028
-
|
PF-02413873
PF-2413873
|
Progesterone Receptor
|
Endocrinology
|
|
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
|
-
- HY-50682
-
|
Azeliragon
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-P1065A
-
|
Apelin-36(rat, mouse) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-P1066A
-
|
Apelin-17(human, bovine) TFA
|
HIV
|
Infection
|
|
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-B0822
-
|
Fipronil
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
|
Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-101249
-
|
L-732138
|
Neurokinin Receptor
|
Cancer
Neurological Disease
|
|
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
|
-
- HY-103409
-
|
ABT-724 trihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
|
-
- HY-15238A
-
-
- HY-P1025
-
-
- HY-N2079
-
-
- HY-P0108
-
-
- HY-N6628
-
-
- HY-14803
-
-
- HY-B0305A
-
-
- HY-U00234
-
-
- HY-103668A
-
-
- HY-A0027
-
-
- HY-B2215
-
-
- HY-B0489
-
-
- HY-14917
-
-
- HY-100255
-
-
- HY-U00139
-
-
- HY-16950
-
-
- HY-16722
-
-
- HY-U00230
-
-
- HY-B0463
-
-
- HY-A0250
-
-
- HY-N2309
-
-
- HY-107480
-
-
- HY-101106
-
-
- HY-14799
-
-
- HY-14864A
-
-
- HY-B0205
-
-
- HY-B1283
-
-
- HY-P0236
-
-
- HY-B1303
-
-
- HY-14864
-
-
- HY-14289
-
-
- HY-101216
-
