Search Result
Results for "Antifolate Antagonists" in MCE Product Catalog:
1801
Inhibitors & Agonists
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-18668
-
-
- HY-19095
-
|
TNP-351
|
Antifolate
|
Cancer
|
|
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
|
-
- HY-10036
-
-
- HY-50159
-
-
- HY-50158
-
-
- HY-128781
-
-
- HY-10446
-
|
Pralatrexate
|
Antifolate
Apoptosis
|
Cancer
|
|
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
|
-
- HY-50713
-
-
- 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-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity.
|
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- HY-129995A
-
-
- HY-131016
-
|
IHR-Cy3
|
Smo
|
Cancer
|
|
IHR-Cy3 is a potent fluorescent Smo antagonist with an IC50 of 100 nM.
|
-
- HY-103009
-
|
MSX-127
|
CXCR
|
Cancer
|
|
MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
|
-
- HY-103010
-
|
MSX-130
|
CXCR
|
Cancer
|
|
MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
|
-
- HY-122136
-
|
S26131
|
Melatonin Receptor
|
Neurological Disease
|
|
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
|
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- HY-14523
-
|
LY 254155
|
Antifolate
|
Cancer
|
|
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
|
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- HY-110303
-
-
- HY-133112
-
-
- HY-13781
-
|
Pemetrexed disodium hemipenta hydrate
LY231514 disodium hemipenta hydrate
|
Antifolate
Autophagy
Apoptosis
|
Cancer
|
|
Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
-
- HY-10820
-
|
Pemetrexed
LY231514
|
Antifolate
Autophagy
|
Cancer
|
|
Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
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- 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).
|
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- 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.
|
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- 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).
|
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- HY-10820A
-
|
Pemetrexed disodium
LY231514 disodium
|
Antifolate
Autophagy
Apoptosis
|
Cancer
|
|
Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
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- HY-107981
-
|
LSN 3213128
|
Antifolate
|
Cancer
|
|
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
|
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- HY-14519
-
|
Methotrexate
Amethopterin; CL14377; WR19039
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- HY-12397
-
|
ZK159222
|
VD/VDR
|
Endocrinology
|
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
|
-
- HY-14519A
-
|
Methotrexate disodium
Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
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- HY-N6932
-
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- HY-17038A
-
|
Agomelatine hydrochloride
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038
-
|
Agomelatine
S-20098
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038B
-
|
Agomelatine (L(+)-Tartaric acid)
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
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- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
|
Cancer
Neurological Disease
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
|
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- HY-103575A
-
|
MFZ 10-7 hydrochloride
|
mGluR
|
Neurological Disease
|
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
|
-
- HY-P1185
-
|
Antagonist G
|
Vasopressin Receptor
Apoptosis
|
Cancer
|
|
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
|
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- HY-100274
-
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- HY-P1185A
-
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- HY-103651
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- HY-129995B
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- HY-111500
-
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- HY-101695
-
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- HY-103652
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- HY-100122
-
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- HY-112562
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- HY-136437
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- HY-112265
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- HY-101264
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- HY-103650
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- HY-18075
-
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- HY-101536
-
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- HY-22437
-
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- HY-U00334
-
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- HY-118844
-
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- HY-112264
-
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- HY-U00330
-
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- HY-B1439B
-
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- HY-107430
-
|
Oxythiamine
Hydroxythiamin
|
Others
|
Cancer
|
|
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
|
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- HY-112262
-
-
- HY-110037
-
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- HY-15015A
-
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- HY-U00375
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- HY-U00320
-
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- HY-U00121
-
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- HY-136152
-
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- HY-100321
-
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- 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.
|
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- HY-111669
-
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- HY-103649
-
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- HY-101704
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- HY-B1205A
-
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- HY-135773
-
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- HY-101915
-
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- HY-U00408
-
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- HY-U00331
-
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- HY-117793
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- HY-112263
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- 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.
|
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- HY-100331
-
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- HY-121186
-
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- HY-15015
-
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- HY-112792
-
-
- HY-110203
-
|
R-7050
TNF-α Antagonist III
|
TNF Receptor
|
Cancer
|
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R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
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- HY-U00360
-
-
- HY-15257A
-
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- HY-U00359
-
-
- HY-104059
-
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- HY-18076
-
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- HY-B0548S1
-
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- HY-100170
-
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- HY-125820
-
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- HY-114193
-
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- HY-114194
-
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- HY-130261
-
-
- HY-117153
-
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- HY-111484
-
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- HY-70002B
-
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- HY-N1163
-
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- HY-126217
-
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- HY-B2111
-
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- HY-N3610
-
|
Coclaurine
|
nAChR
|
Neurological Disease
|
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
|
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- HY-111443
-
-
- HY-B1505
-
-
- HY-100248
-
-
- HY-Z0816
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-32329A
-
-
- HY-P2268
-
|
RAGE antagonist peptide
|
Amyloid-β
|
|
|
RAGE antagonist peptide is an antagonist of Receptor for advanced glycation end products (RAGE). RAGE blocks S100P, S100A4 and HMGB-1 mediated RAGE activation. RAGE antagonist peptide inhibits growth and metastasis of rat glioma tumors. RAGE antagonist peptide also reduces cell growth and RAGE-mediated NF-κB activity in human PDAC cell lines.
|
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- HY-112430
-
-
- HY-U00368
-
-
- HY-100261
-
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- HY-15540
-
-
- HY-111494
-
-
- HY-125970
-
-
- HY-136459
-
|
NMDA receptor antagonist 2
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
|
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- HY-129357
-
-
- HY-100648
-
-
- HY-100649
-
-
- HY-16991
-
-
- HY-B1547A
-
-
- HY-100266
-
-
- HY-B0561
-
-
- HY-U00067
-
-
- HY-101685
-
-
- HY-103456
-
-
- HY-114017
-
-
- HY-108323
-
|
CCR2 antagonist 4
Teijin compound 1
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-103362
-
|
CCR2 antagonist 4 hydrochloride
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-15066
-
|
CNQX
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
|
-
- HY-113973
-
|
LPA2 antagonist 2
|
LPL Receptor
|
Cancer
|
|
LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).
|
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- HY-136220
-
|
AHR antagonist 5
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
|
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- HY-129946
-
-
- HY-124759
-
-
- HY-112056
-
-
- HY-15277
-
-
- HY-U00365
-
-
- HY-13242
-
|
Taladegib
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
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- HY-B0661
-
-
- HY-10053
-
-
- HY-15372
-
-
- HY-17498
-
-
- HY-106910
-
-
- HY-100850
-
-
- HY-12525
-
-
- HY-19223
-
-
- HY-15067
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-
- HY-B0461
-
-
- HY-100903
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-
- HY-101106
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-
- HY-U00110
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-
- HY-B1589A
-
-
- HY-101574
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-
- HY-U00017
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-
- HY-101594
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-
- HY-U00062
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-
- HY-101675
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-
- HY-101691
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-
- HY-B1240
-
-
- HY-105117
-
-
- HY-B0480
-
-
- HY-102024
-
-
- HY-U00321
-
-
- HY-70050AS
-
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- HY-B0524A
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-
- HY-120588
-
-
- HY-U00397
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-
- HY-101913
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-
- HY-12195
-
-
- HY-U00286
-
-
- HY-U00322
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-
- HY-15066A
-
|
CNQX disodium
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
|
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- HY-19638A
-
|
Cangrelor tetrasodium
|
P2Y Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
|
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- HY-111755
-
-
- HY-19818A
-
-
- HY-128878
-
-
- HY-19705B
-
-
- HY-N2189
-
-
- HY-130992
-
-
- HY-101534
-
-
- HY-109139
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-
- HY-B0768A
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-
- HY-U00245
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-
- HY-13202
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-
- HY-100255
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-
- HY-U00202
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-
- HY-B0460
-
-
- HY-100173
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-
- HY-15068
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-
- HY-N0219
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-
- HY-100714A
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-
- HY-B1014
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-
- HY-103531
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-
- HY-P0262
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-
- HY-101707
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-
- HY-B1303A
-
-
- HY-13209
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-
- HY-P1329
-
-
- HY-B2154
-
-
- HY-G0014
-
|
Quetiapine sulfoxide
Quetiapine S-oxide
|
Drug Metabolite
|
Neurological Disease
|
|
Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.
|
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- HY-G0014B
-
-
- HY-G0014A
-
-
- HY-U00353
-
-
- HY-111449
-
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- 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.
|
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- HY-17039S
-
-
- HY-125819
-
-
- 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-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
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- HY-P1025
-
-
- HY-N2079
-
-
- HY-19121A
-
-
- HY-U00247
-
-
- HY-A0082
-
-
- HY-N6628
-
-
- HY-B0305A
-
-
- HY-U00234
-
-
- HY-A0027
-
-
- HY-16168A
-
-
- HY-U00139
-
-
- HY-19737A
-
-
- HY-A0250
-
-
- HY-B1165
-
-
- HY-B0462A
-
-
- HY-B0548
-
-
- HY-B0548A
-
-
- HY-B0205
-
-
- HY-B1283
-
-
- HY-P1329A
-
-
- HY-B0251
-
-
- HY-B1303
-
-
- HY-103184
-
-
- HY-66012
-
-
- HY-100668
-
-
- HY-14289
-
-
- HY-B0325
-
-
- HY-16635
-
-
- HY-B0323
-
-
- HY-10164
-
-
- HY-U00119
-
-
- HY-100292
-
-
- HY-15539
-
-
- HY-101743
-
-
- HY-B0547A
-
-
- HY-B0286A
-
-
- HY-101906
-
-
- HY-B0462
-
-
- HY-100191
-
-
- HY-110254
-
-
- HY-U00040
-
-
- HY-106659
-
-
- HY-130845
-
|
AR antagonist 1
|
Ligand for E3 Ligase
|
Cancer
|
|
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
|
-
- HY-116649
-
-
- HY-P0107
-
-
- HY-B1301
-
-
- HY-P0107B
-
-
- HY-133123
-
-
- HY-135830
-
|
AHR antagonist 4
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects.
|
-
- HY-111501
-
-
- HY-19733
-
-
- 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-135831
-
|
AHR antagonist 2
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR.
|
-
- HY-131256
-
-
- HY-110110
-
-
- HY-15085
-
-
- HY-17037
-
-
- HY-U00350
-
-
- HY-100454
-
-
- HY-19732
-
-
- HY-12710A
-
-
- HY-112620
-
-
- HY-16763
-
-
- HY-16732
-
-
- HY-B0429
-
-
- HY-B0009
-
-
- HY-B0241
-
-
- HY-A0066
-
-
- HY-13315
-
-
- HY-U00019
-
-
- HY-101600
-
-
- HY-101745
-
-
- HY-101618
-
-
- HY-B0895
-
-
- HY-18689
-
-
- HY-B1164
-
-
- HY-17465
-
-
- HY-18555
-
|
TMPA
|
Others
|
Others
|
|
TMPA is an antagonist of nuclear receptor Nur77 and LKB1 interaction.
|
-
- HY-12503
-
-
- HY-18101A
-
-
- HY-13831
-
-
- HY-14656
-
-
- HY-112248
-
-
- HY-P0107A
-
-
- HY-112730
-
|
PEO-IAA
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-100405
-
|
FTIDC
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
|
-
- HY-125836
-
|
CCR4 antagonist 2
|
CCR
|
Cancer
Endocrinology
|
|
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
|
-
- HY-14276A
-
|
Gallopamil hydrochloride
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-14276
-
|
Gallopamil
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-102004
-
-
- HY-102037
-
-
- HY-42849
-
-
- HY-B0281A
-
-
- HY-15487
-
-
- HY-14778
-
-
- HY-17582
-
-
- HY-B0310
-
-
- HY-15001
-
-
- HY-100471
-
-
- HY-102093
-
-
- HY-B2168
-
-
- HY-101502A
-
-
- HY-B0004
-
-
- HY-P0009A
-
-
- HY-14538A
-
-
- HY-P0061
-
-
- HY-13439
-
-
- HY-12114
-
-
- HY-50663
-
-
- HY-42849A
-
-
- HY-109077
-
-
- HY-101797
-
-
- HY-15758
-
-
- HY-U00018
-
-
- HY-101632
-
-
- HY-19243
-
-
- HY-101668
-
-
- HY-15105
-
-
- HY-101679
-
-
- HY-19163
-
-
- HY-15073
-
-
- HY-P0209
-
-
- HY-103099
-
-
- HY-100153
-
-
- HY-14284
-
-
- HY-14538
-
-
- HY-114191
-
-
- 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-114191A
-
-
- HY-101116
-
-
- HY-100607A
-
-
- HY-A0066A
-
-
- HY-17492
-
-
- HY-B0774
-
-
- HY-14859
-
-
- HY-13021
-
-
- HY-76520
-
-
- HY-15709
-
-
- HY-110095
-
-
- HY-112604
-
-
- HY-15574
-
-
- HY-B0321
-
-
- HY-15108
-
-
- HY-B0128
-
-
- HY-12380
-
-
- HY-B1108
-
-
- HY-101177
-
-
- HY-14369
-
-
- HY-16509
-
-
- HY-107765
-
-
- HY-12380A
-
-
- HY-B0569
-
-
- HY-112703
-
-
- HY-14130
-
-
- HY-B0205S
-
-
- HY-10486
-
-
- HY-A0075
-
-
- HY-B2073A
-
-
- HY-16701
-
|
BV6
|
IAP
|
Cancer
|
|
BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
|
-
- HY-B0362A
-
-
- HY-12510
-
-
- HY-P0264
-
-
- HY-U00289
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-B2073
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-101706
-
-
- HY-101830
-
-
- HY-101721
-
-
- HY-U00283
-
-
- HY-14367
-
-
- HY-G0012
-
-
- HY-U00257
-
-
- HY-U00404
-
-
- HY-103533
-
-
- HY-U00188
-
-
- HY-U00207
-
-
- HY-135976
-
|
P2X3 antagonist 34
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
|
-
- HY-N0096
-
-
- HY-103213
-
-
- HY-103200
-
-
- HY-16474
-
|
Relugolix
TAK-385
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.
|
-
- HY-100672
-
-
- HY-12881
-
|
Eliprodil
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-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-13706A
-
|
CAY10471
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.
|
-
- 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-U00443
-
-
- HY-17001
-
-
- HY-B0192A
-
-
- HY-B0160
-
-
- HY-B0192
-
-
- HY-U00263
-
-
- HY-B0682A
-
-
- HY-10259
-
-
- HY-16692
-
-
- HY-U00253
-
-
- HY-19768
-
-
- HY-10413
-
-
- HY-13541
-
|
ADH-1
|
Others
|
Cancer
|
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-14423
-
-
- HY-12426
-
-
- HY-A0033
-
-
- HY-B1487
-
-
- HY-B0500
-
-
- HY-B0298A
-
-
- HY-U00212
-
-
- HY-B0366A
-
-
- HY-11103
-
-
- HY-14770
-
-
- HY-108324
-
-
- HY-10259A
-
-
- HY-G0011
-
-
- HY-U00363
-
-
- HY-12799
-
-
- HY-N1378
-
-
- HY-14447
-
-
- HY-B0369A
-
-
- HY-B0412
-
-
- HY-A0145
-
|
Phenprocoumon
|
Others
|
Others
|
|
Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
|
-
- HY-U00335
-
-
- HY-17001A
-
-
- HY-15574A
-
-
- HY-10414
-
-
- HY-19670
-
-
- HY-101683
-
-
- HY-14129
-
-
- HY-19855
-
-
- HY-50912
-
-
- HY-101718
-
-
- HY-15702
-
|
HJC0350
|
Others
|
Cancer
|
|
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
|
-
- HY-15640
-
-
- HY-13004
-
-
- HY-118861A
-
-
- HY-14432
-
-
- HY-50691
-
-
- HY-100382
-
|
FPTQ
|
mGluR
|
Others
|
|
FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively.
|
-
- HY-101407
-
-
- HY-B0781
-
-
- 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-N0607
-
-
- HY-103360
-
|
J-113863
|
CCR
|
Inflammation/Immunology
|
|
J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.
|
-
- HY-A0019A
-
|
Paliperidone palmitate
9-Hydroxyrisperidone palmitate
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.
|
-
- HY-15403
-
-
- HY-13541A
-
-
- HY-B1438
-
-
- HY-111442
-
|
GC 14
|
Others
|
Metabolic Disease
|
|
GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
|
-
- HY-112667
-
-
- HY-100318
-
-
- HY-16502
-
|
Transcrocetinate disodium
Disodium trans-crocetinate
|
iGluR
|
Cancer
|
|
Transcrocetinate disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-14538S
-
-
- HY-19904
-
-
- HY-B1517A
-
-
- HY-B0355
-
-
- HY-P1558
-
-
- HY-10560
-
-
- HY-101527
-
|
20-HEDE
WIT 002
|
Others
|
Cancer
|
|
20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
|
-
- HY-17512
-
-
- HY-U00356
-
-
- HY-112050
-
-
- HY-U00392
-
-
- HY-B0539
-
-
- HY-19057A
-
-
- HY-19632
-
-
- HY-B0716
-
-
- HY-16756
-
-
- HY-19193
-
-
- HY-100152
-
-
- HY-18611A
-
-
- HY-14609
-
-
- HY-B0391
-
-
- HY-50669
-
-
- HY-110136A
-
-
- HY-U00251
-
-
- HY-42937
-
|
Transcrocetin meglumine salt
trans-Crocetin meglumine salt
|
iGluR
|
Cancer
|
|
Transcrocetin meglumine salt, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-B1517
-
-
- HY-105018
-
|
Epelsiban
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-10052
-
-
- HY-10088
-
-
- HY-19914
-
-
- HY-U00252
-
-
- HY-12752A
-
-
- HY-B1510
-
-
- HY-19654
-
-
- HY-18611
-
-
- HY-101620
-
-
- HY-19909
-
|
NRC-2694
|
EGFR
|
Cancer
|
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-101700
-
-
- HY-U00076
-
-
- HY-17505
-
-
- HY-B1225
-
-
- HY-111398
-
-
- HY-15853
-
-
- HY-12377
-
-
- HY-110136
-
-
- HY-14538S1
-
-
- HY-13796
-
-
- HY-N2332A
-
-
- HY-15319B
-
-
- HY-100308
-
-
- HY-114452
-
|
LY-2940094
|
Opioid Receptor
|
Neurological Disease
|
|
LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models.
|
-
- 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-14263
-
|
Pericyazine
Propericiazine; RP 8909
|
Dopamine Receptor
|
Neurological Disease
|
|
Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.
|
-
- HY-100703
-
-
- HY-112629
-
-
- HY-112558
-
-
- HY-N0184
-
-
- HY-P0171
-
-
- HY-W014325
-
-
- HY-50669A
-
-
- HY-50175
-
-
- HY-A0012
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-18697
-
-
- HY-15577
-
|
GSK3787
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-15195
-
-
- HY-B0478
-
-
- HY-12635
-
-
- HY-12426A
-
-
- HY-13059B
-
-
- HY-10995
-
-
- HY-P1014
-
-
- HY-U00106
-
-
- HY-114025
-
-
- HY-B1435
-
-
- HY-108688
-
-
- HY-13059
-
-
- HY-15403A
-
-
- HY-B0549A
-
-
- HY-18966
-
-
- HY-15411
-
-
- HY-120090
-
-
- HY-19391
-
-
- HY-18204
-
-
- HY-B0325S
-
-
- HY-118180
-
-
- HY-14407
-
-
- HY-U00084
-
-
- HY-12131
-
-
- HY-19274
-
-
- HY-101669
-
-
- HY-19969
-
-
- HY-13100
-
-
- HY-15541
-
-
- HY-118678
-
-
- HY-B0909
-
-
- HY-10064
-
-
- HY-14751
-
-
- HY-108997
-
-
- HY-P1572
-
-
- HY-B1126
-
-
- HY-B1613A
-
-
- HY-12715
-
-
- HY-15129
-
|
O-Phospho-L-serine
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
|
-
- HY-16978
-
-
- HY-100692
-
|
Lin28-let-7a antagonist 1
|
MicroRNA
|
Cancer
|
|
Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
|
-
- HY-15084
-
-
- HY-103407A
-
-
- HY-12339
-
|
NVS-CRF38
|
CRFR
|
Endocrinology
|
|
NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
|
-
- HY-B0538A
-
-
- HY-U00433
-
-
- HY-14336A
-
-
- HY-13059A
-
-
- HY-120689
-
-
- HY-50674A
-
-
- HY-B0431A
-
-
- HY-W018061
-
-
- HY-B1081
-
-
- HY-19347
-
-
- HY-15462
-
-
- HY-12765S
-
-
- HY-13534
-
-
- HY-103454
-
-
- HY-B0661A
-
-
- HY-14338A
-
-
- HY-100882
-
-
- HY-10634
-
-
- HY-13282
-
|
GANT 58
NSC 75503
|
Gli
|
Cancer
|
|
GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
|
-
- HY-19489S
-
-
- HY-110255
-
-
- HY-101105A
-
-
- HY-B0202
-
-
- HY-14914
-
-
- HY-B0780
-
-
- HY-10655
-
-
- HY-17024
-
-
- HY-15835
-
|
CUDC-427
GDC-0917
|
IAP
|
Cancer
|
|
CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
|
-
- HY-14338
-
-
- HY-12428
-
-
- HY-U00402
-
-
- HY-12127
-
-
- HY-U00077
-
-
- HY-19191
-
-
- HY-19110
-
-
- HY-14938
-
-
- HY-14407A
-
-
- HY-112710
-
-
- HY-U00105
-
-
- HY-107437
-
-
- HY-B1305
-
-
- HY-U00143
-
-
- HY-125879
-
-
- HY-N0145
-
-
- HY-12777
-
-
- HY-U00354
-
-
- HY-12301
-
-
- HY-103430
-
|
SKF-83566 hydrobromide
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo.
|
-
- HY-14561A
-
|
Idazoxan hydrochloride
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
|
-
- 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-110279
-
|
Ogerin
|
Others
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
|
-
- HY-P1017
-
-
- HY-50901
-
-
- HY-15009
-
-
- HY-112596A
-
-
- HY-128351
-
-
- HY-19512
-
-
- HY-100717
-
-
- HY-15726
-
-
- HY-A0024
-
|
Tolterodine
(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
|
mAChR
|
Neurological Disease
|
|
Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-P0216
-
-
- HY-19736
-
-
- HY-19654B
-
-
- HY-B1059
-
-
- HY-16023A
-
-
- HY-B0595
-
-
- HY-W040146
-
-
- HY-13575
-
-
- HY-100129
-
-
- HY-10900
-
-
- HY-113534
-
|
MV1
|
IAP
|
Others
|
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
|
-
- HY-A0018
-
-
- HY-17390
-
-
- HY-112596
-
-
- HY-A0163
-
-
- HY-10487
-
-
- HY-13683
-
-
- HY-112895
-
|
UT-155
|
Androgen Receptor
|
Cancer
|
|
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
|
-
- HY-16346
-
-
- HY-100372
-
-
- HY-A0013A
-
-
- HY-15257
-
|
Mavoglurant
AFQ056
|
mGluR
|
Neurological Disease
|
|
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.
|
-
- HY-14951
-
-
- HY-101638
-
-
- HY-19097
-
-
- HY-19048
-
-
- HY-19499
-
-
- HY-19025
-
-
- HY-U00028
-
-
- HY-112284
-
-
- HY-U00237
-
-
- HY-A0013
-
-
- HY-101953
-
-
- HY-17390A
-
-
- HY-B0354A
-
-
- HY-P0061A
-
-
- 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-14467
-
-
- HY-12949
-
-
- 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-15538
-
-
- HY-15419
-
-
- HY-N4247
-
-
- HY-70050C
-
-
- HY-135363
-
-
- HY-16993
-
-
- HY-101986
-
-
- HY-108251
-
-
- HY-101486
-
|
LF3
|
β-catenin
|
Cancer
|
|
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
|
-
- HY-12506A
-
|
Naspm trihydrochloride
1-Naphthylacetyl spermine trihydrochloride
|
iGluR
|
Neurological Disease
|
|
Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
|
-
- HY-13535
-
|
ATN-161
|
Integrin
|
Cancer
|
|
ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
|
-
- HY-17398
-
-
- HY-16985
-
|
Darolutamide
ODM-201; BAY-1841788
|
Androgen Receptor
|
Cancer
|
|
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
|
-
- HY-13604
-
-
- HY-P1276
-
-
- HY-70050A
-
-
- HY-B0686
-
-
- HY-15851
-
-
- HY-101503
-
|
HTS01037
|
FABP
|
Metabolic Disease
|
|
HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- 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-U00302
-
-
- HY-12780S
-
-
- HY-N0382
-
|
Galangin
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-A0021
-
-
- HY-P1727A
-
|
Super-TDU TFA
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist therapy against gastric cancer targeting YAP-TEADs interaction.
|
-
- HY-100209
-
|
Sufugolix
TAK-013
|
Others
|
Endocrinology
|
|
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
|
-
- HY-U00137
-
-
- HY-17039
-
-
- HY-104020A
-
-
- 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-16060
-
-
- HY-19900
-
-
- HY-101395
-
-
- HY-13535A
-
-
- HY-B0686A
-
-
- HY-12142
-
-
- HY-13534A
-
-
- HY-U00382
-
-
- HY-101720
-
|
Fradafiban
BIBU-52
|
Integrin
|
Cardiovascular Disease
|
|
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-101598
-
-
- HY-19189
-
-
- HY-101686
-
-
- HY-101022
-
-
- HY-17351
-
-
- HY-10888
-
-
- HY-14789
-
|
(R)-Elagolix
NBI-56418
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
|
-
- HY-18263A
-
|
Elubrixin
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation.
|
-
- HY-13222
-
-
- HY-B1510S
-
-
- HY-B0071
-
-
- HY-12506
-
|
Naspm
1-Naphthylacetyl spermine
|
iGluR
|
Neurological Disease
|
|
Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
|
-
- HY-14551
-
-
- HY-N0127
-
-
- HY-12378
-
-
- HY-16040
-
-
- HY-B1081A
-
-
- HY-B0394
-
-
- HY-18287
-
|
MRT-83
|
Smo
|
Cancer
|
|
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
|
-
- HY-B0674
-
-
- HY-14782
-
-
- HY-101586
-
-
- HY-107735
-
-
- HY-17428
-
-
- HY-50081
-
-
- HY-12488
-
-
- HY-109002
-
-
- HY-70002
-
-
- HY-12940
-
-
- HY-111539
-
-
- HY-B0750
-
|
Dolasetron
MDL-73147
|
5-HT Receptor
|
Others
|
|
Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
|
-
- HY-15370
-
-
- HY-19205A
-
-
- HY-17000
-
-
- HY-101844
-
-
- HY-14537
-
-
- HY-109593
-
-
- HY-16683
-
-
- HY-18347A
-
-
- HY-14914S
-
-
- HY-16682
-
|
AGN 196996
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
|
-
- HY-U00341
-
-
- HY-B0071A
-
-
- HY-104003
-
-
- HY-14609A
-
|
MPEP
|
mGluR
|
Neurological Disease
|
|
MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
|
-
- HY-101833
-
|
YM-264
|
Others
|
Inflammation/Immunology
|
|
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
|
-
- HY-101809
-
-
- HY-101815
-
-
- HY-19062
-
-
- HY-15853A
-
-
- HY-16582A
-
|
Sonidegib
Erismodegib; LDE225; NVP-LDE225
|
Smo
|
Cancer
|
|
Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
|
-
- HY-15481
-
-
- HY-105545
-
|
Dexetimide
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
|
mAChR
|
Cardiovascular Disease
|
|
Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
|
-
- HY-B0202S
-
-
- HY-108690
-
|
Fluxametamide
|
GABA Receptor
|
Others
|
|
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
|
-
- HY-B1494
-
-
- HY-A0125A
-
-
- HY-P1309A
-
-
- HY-B0031S
-
-
- HY-16312
-
|
MDL-29951
|
iGluR
|
Neurological Disease
|
|
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
|
-
- HY-101458
-
-
- HY-P1869
-
-
- HY-101910
-
-
- HY-13505
-
-
- 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-135588
-
-
- HY-10794
-
-
- HY-15418
-
-
- HY-16697
-
|
CID 16020046
|
GPR55
|
Cancer
|
|
CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.
|
-
- HY-15443
-
-
- HY-15676
-
-
- HY-13677
-
-
- HY-U00185
-
-
- HY-13466
-
-
- HY-17360
-
|
Tiotropium Bromide
BA679 BR
|
mAChR
|
Neurological Disease
|
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-119217
-
-
- HY-P1479
-
-
- HY-10857
-
-
- HY-10889
-
-
- HY-112840
-
-
- HY-17004
-
-
- HY-10792
-
-
- HY-17512S
-
-
- HY-101226
-
|
MSOP
|
mGluR
|
Neurological Disease
|
|
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
|
-
- HY-15488
-
-
- HY-B0303A
-
-
- HY-B0068
-
-
- HY-15653
-
-
- HY-12366
-
-
- HY-17436
-
-
- HY-101736
-
|
AMG9810
|
TRP Channel
|
Neurological Disease
|
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
|
-
- HY-103228
-
-
- HY-103361
-
-
- HY-14825
-
|
Tarafenacin
SVT-40776
|
mAChR
|
Neurological Disease
|
|
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-133570
-
|
17-AEP-GA
|
HSP
ADC Cytotoxin
|
Cancer
|
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
|
-
- HY-10388
-
-
- HY-U00117
-
-
- HY-B0322
-
|
Sulfamethoxazole
Ro 4-2130
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonists of para-aminobenzoic acid (PABA).
|
-
- HY-15488A
-
-
- HY-B0377
-
-
- HY-103449
-
-
- HY-101727
-
-
- HY-101619
-
-
- HY-19477
-
-
- 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-13508
-
-
- HY-15722
-
-
- HY-101458A
-
-
- HY-112693
-
|
H-151
|
STING
|
Inflammation/Immunology
|
|
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.
|
-
- HY-U00238
-
-
- HY-13274
-
-
- HY-15724
-
|
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK-1605786) is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
|
-
- HY-15799
-
-
- HY-10633
-
-
- HY-17407
-
-
- HY-14791A
-
-
- HY-19989A
-
-
- HY-112202
-
-
- HY-B0750B
-
-
- HY-15421
-
-
- HY-15834A
-
-
- HY-16346S
-
-
- HY-16578
-
|
GW9662
|
PPAR
|
Cancer
|
|
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
|
-
- HY-17512A
-
-
- HY-17621
-
-
- 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-13331
-
|
Clascoterone
Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-133080
-
|
BAY-784
|
GNRH Receptor
|
Cancer
|
|
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
|
-
- HY-10871A
-
-
- HY-14542A
-
-
- HY-B0750A
-
-
- HY-135103
-
|
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- 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-14144
-
|
Aclidinium Bromide
LAS 34273; LAS-W 330
|
mAChR
|
Inflammation/Immunology
|
|
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
|
-
- HY-13245
-
-
- HY-16582
-
|
Sonidegib diphosphate
Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate
|
Smo
|
Cancer
|
|
Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
|
-
- HY-P1203
-
-
- HY-10871
-
-
- HY-70002S
-
-
- HY-19084
-
|
Ro-24-0238
|
Others
|
Inflammation/Immunology
|
|
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
|
-
- HY-19214
-
-
- HY-136596
-
|
Apalutamide-COOH
|
Others
|
Cancer
|
|
Apalutamide-COOH can be used to synthesis Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
|
-
- HY-U00449
-
|
AGN 193109
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
|
-
- HY-17458
-
-
- HY-100409
-
|
PHCCC
|
mGluR
|
Cancer
|
|
PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
|
-
- HY-100619
-
|
BMS-986020
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-19627
-
|
Naldemedine
S-297995
|
Opioid Receptor
|
Neurological Disease
|
|
Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia.
|
-
- HY-B1716
-
|
L-5-Hydroxytryptophan
L-5-HTP; Oxitriptan
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia.
|
-
- HY-100619A
-
|
BMS-986020 sodium
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-P1750
-
|
Shepherdin (79-87)
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
|
-
- HY-10418
-
-
- HY-100720
-
-
- HY-50697
-
-
- HY-17497A
-
-
- HY-14736
-
-
- HY-P1276A
-
-
- HY-15708
-
-
- HY-117819
-
|
TMP920
|
ROR
|
Inflammation/Immunology
|
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-P1203A
-
-
- 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-109103
-
|
Tegatrabetan
BC2059
|
β-catenin
|
Cancer
|
|
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
|
-
- HY-12190A
-
-
- HY-13243
-
|
Alvimopan
ADL 8-2698; LY 246736
|
Opioid Receptor
|
Metabolic Disease
|
|
Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
|
-
- HY-14121
-
-
- HY-B0164A
-
-
- HY-12005
-
-
- HY-17410A
-
-
- HY-16996A
-
-
- HY-107382
-
-
- HY-U00355
-
-
- HY-16711
-
-
- 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-U00433A
-
-
- HY-14880B
-
-
- HY-107723
-
-
- HY-119433
-
|
Asoprisnil
J867
|
Progesterone Receptor
|
Endocrinology
|
|
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
|
-
- HY-76657A
-
|
Alvimopan dihydrate
ADL 8-2698 dihydrate; LY 246736 dihydrate
|
Opioid Receptor
|
Neurological Disease
|
|
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
|
-
- HY-B0164
-
-
- HY-I0021
-
-
- HY-10564
-
-
- HY-A0002
-
-
- HY-N0184B
-
-
- HY-19902
-
-
- HY-B1270
-
-
- HY-100562
-
-
- HY-B1486
-
-
- HY-101385
-
-
- HY-76657
-
|
Alvimopan monohydrate
ADL 8-2698 monohydrate; LY 246736 monohydrate
|
Opioid Receptor
|
Neurological Disease
|
|
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
|
-
- HY-14339
-
-
- HY-109987
-
|
ISPA-28
|
Parasite
|
Infection
|
|
ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3.
|
-
- HY-12190
-
-
- HY-111271A
-
-
- HY-B1541
-
-
- HY-14542S
-
-
- HY-U00151
-
-
- HY-13713
-
-
- HY-U00072
-
-
- HY-15894
-
-
- HY-100760
-
|
Toxoflavin
Xanthothricin; Toxoflavine; PKF-118-310
|
β-catenin
|
Cancer
|
|
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
|
-
- HY-10561
-
|
RU 58841
PSK-3841; HMR-3841
|
Androgen Receptor
|
Endocrinology
|
|
RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.
|
-
- HY-131277
-
-
- HY-B1655
-
|
Fluspirilene
R 6218; Redeptin
|
Calcium Channel
|
Neurological Disease
|
|
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
|
-
- HY-14880
-
-
- HY-11029
-
-
- HY-107382A
-
-
- HY-16704
-
|
ESI-09
|
Virus Protease
|
Cancer
|
|
ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
|
-
- HY-17410
-
-
- HY-B0407A
-
-
- HY-12497
-
-
- HY-116790A
-
-
- HY-14880A
-
-
- HY-13556A
-
|
Arzoxifene hydrochloride
LY 353381 HCl; SERM 3
|
Estrogen Receptor/ERR
|
Cancer
|
|
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
|
-
- HY-101690
-
-
- HY-115506
-
-
- HY-B0031S1
-
-
- HY-15950
-
-
- HY-107649
-
|
Zamifenacin fumarate
UK-76654 fumarate
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
|
-
- HY-14875
-
-
- HY-10388A
-
-
- 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-131278
-
-
- HY-13527
-
-
- HY-14545A
-
-
- HY-75766S
-
-
- 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-U00189
-
-
- HY-101924
-
-
- HY-17497S
-
-
- HY-10013A
-
-
- HY-10011
-
-
- HY-A0084
-
|
Procainamide hydrochloride
|
Autophagy
|
Cancer
|
|
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
|
-
- HY-101336
-
-
- HY-B0002B
-
|
Ondansetron
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron(GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-101430
-
-
- HY-14567
-
-
- HY-11063
-
-
- 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-19532
-
-
- HY-13206
-
|
MTEP hydrochloride
|
mGluR
|
Neurological Disease
|
|
MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride produces antiparkinsonian-like effects.
|
-
- HY-12336
-
-
- HY-12981
-
-
- HY-30152
-
-
- HY-120261
-
-
- HY-123337
-
|
Zamifenacin
UK-76654
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
|
-
- HY-14545
-
-
- HY-17446
-
-
- HY-U00425
-
-
- HY-18204S
-
-
- 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-Y0313
-
-
- HY-N0546
-
|
Ligustroflavone
Nuezhenoside
|
CaSR
|
Metabolic Disease
|
|
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice.
|
-
- HY-B0002
-
|
Ondansetron hydrochloride
GR 38032 hydrochloride; SN 307 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron hydrochloride (GR 38032 hydrochloride; SN 307 hydrochloride) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-B0437
-
-
- HY-108896
-
-
- HY-100316
-
-
- HY-10562
-
-
- HY-124754
-
|
BTRX-335140
CYM-53093
|
Opioid Receptor
|
Metabolic Disease
|
|
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) .
|
-
- HY-109067
-
|
Opiranserin
|
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
|
-
- HY-P1267
-
|
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-110123
-
-
- HY-101348
-
-
- HY-135589
-
-
- HY-13955
-
-
- HY-108329
-
-
- HY-100208
-
|
HC-067047
|
TRP Channel
|
Cancer
|
|
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
|
-
- HY-13636B
-
|
Fulvestrant (R enantiomer)
ICI 182780 (R enantiomer); ZD 9238 (R enantiomer); ZM 182780 (R enantiomer)
|
Others
|
Cancer
|
|
Fulvestrant R enantiomer (ICI 182780 R enantiomer; ZD 9238 R enantiomer; ZM 182780 R enantiomer) is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-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-131276
-
-
- HY-N0471A
-
|
L-Hyoscyamine sulfate
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate) is a tropane alkaloid that is a secondary metabolite found in certain plants of the solanaceae family. In vitro it has been shown to be an antagonist of mAChR.
|
-
- HY-103088
-
-
- HY-14365
-
-
- HY-A0015
-
-
- HY-B0115
-
-
- HY-101381
-
|
Otenzepad
AF-DX 116
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
|
-
- HY-110322A
-
|
PPTN
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. Anti-inflammatory and immune activity.
|
-
- HY-15568A
-
-
- HY-N7067
-
|
Revaprazan hydrochloride
|
Bacterial
COX
|
Infection
|
|
Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection.
|
-
- HY-70068
-
-
- HY-14825A
-
-
- HY-P1233
-
-
- 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-101978
-
|
CPI-444
V81444; ciforadenant
|
Adenosine Receptor
|
Cancer
|
|
CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
|
-
- HY-120478
-
|
ASP6432
|
LPL Receptor
|
Infection
|
|
ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively.
|
-
- HY-131274
-
|
Fexofenadine Impurity F
|
Others
|
Others
|
|
Fexofenadine Impurity F is the impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
|
-
- HY-N2064
-
|
Racanisodamine
|
mAChR
|
Neurological Disease
|
|
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control.
|
-
- HY-U00423
-
-
- HY-100183
-
-
- HY-120691A
-
-
- HY-B0548S
-
-
- 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-108136A
-
|
Bisindolylmaleimide X hydrochloride
BIM-X hydrochloride; Ro31-8425 hydrochloride
|
PKC
CDK
|
Cardiovascular Disease
|
|
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
|
-
- HY-13951
-
-
- 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-10806
-
-
- HY-111534
-
|
SBI-115
|
GPCR19
|
Others
|
|
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
|
-
- HY-15568
-
-
- 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-121450
-
|
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-10017
-
|
SCH 546738
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
|
-
- HY-13677A
-
|
6-Mercaptopurine hydrate
Mercaptopurine hydrate; 6-MP hydrate
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
6-Mercaptopurine hydrate (Mercaptopurine hydrate; 6-MP hydrate) is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
|
-
- HY-B0548AS
-
-
- HY-13636A
-
|
Fulvestrant (S enantiomer)
ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)
|
Others
|
Cancer
|
|
Fulvestrant S enantiomer (ICI 182780 S enantiomer; ZD 9238 S enantiomer; ZM 182780 S enantiomer) is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-133555
-
-
- HY-17617
-
-
- HY-108689
-
|
Broflanilide
|
GABA Receptor
|
Neurological Disease
|
|
Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
|
-
- HY-131279
-
|
Olmesartan ethyl ester
|
Others
|
Others
|
|
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study.
|
-
- HY-P1187
-
|
HSDVHK-NH2
|
Integrin
|
Cancer
|
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
|
-
- HY-70050CS
-
-
- HY-15289
-
-
- HY-131255
-
-
- HY-B0532A
-
-
- HY-N0215
-
|
L-Phenylalanine
(S)-2-Amino-3-phenylpropionic acid
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca + channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
|
-
- HY-N3945
-
|
Glaucine
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
|
-
- HY-12707
-
-
- HY-A0081
-
-
- HY-19456
-
-
- HY-107702
-
|
CGP 37849
|
iGluR
|
Neurological Disease
|
|
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects.
|
-
- HY-112302
-
-
- HY-14111
-
-
- HY-50665
-
|
LY518674
LY-674
|
PPAR
|
Metabolic Disease
|
|
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis.
|
-
- HY-10805A
-
-
- HY-121599
-
|
CGP 36742
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression.
|
-
- HY-103316
-
|
trans-Ned 19
|
Calcium Channel
|
Cardiovascular Disease
|
|
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
|
-
- HY-U00367
-
-
- HY-P1187A
-
|
HSDVHK-NH2 TFA
|
Integrin
|
Cancer
|
HSDVHK-NH2 TFA is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
|
-
- HY-12789
-
|
Etrasimod
APD334
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
|
-
- HY-10562A
-
-
- HY-B1986
-
|
p,p'-DDE
4,4'-DDE; p,p'-Dichlorodiphenyldichloroethylene
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
|
p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM.
|
-
- 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-10898
-
-
- HY-10805
-
-
- HY-B0716S
-
-
- HY-15043
-
-
- HY-17004S
-
-
- HY-76612
-
-
- HY-P1267A
-
|
α-Conotoxin PnIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-P1104A
-
|
FC131 TFA
|
CXCR
HIV
|
Infection
|
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
|
-
- HY-124543
-
-
- HY-133775
-
-
- HY-109024
-
-
- HY-N0079
-
-
- HY-N6066
-
-
- HY-108841
-
|
Anakinra
Raleukin; AMG-719
|
Others
|
Cancer
Inflammation/Immunology
|
|
Anakinra (Raleukin) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Anakinra is the first biological agent to block the pro-inflammatory effects.
|
-
- HY-12100
-
-
- 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-10302
-
-
- HY-14185
-
-
- HY-16617
-
|
Auglurant
VU0424238
|
mGluR
|
Neurological Disease
|
|
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
|
-
- HY-112359
-
|
C-82
|
β-catenin
Wnt
|
Cancer
|
|
C-82 is a second-generation specific CBP/β-catenin antagonist, which inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
|
-
- HY-135329
-
|
Solifenacin D5 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- 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-100783A
-
|
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-102023
-
|
GNF351
|
Aryl Hydrocarbon Receptor
|
Others
|
|
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
|
-
- HY-B0801A
-
-
- HY-108912
-
-
- HY-16060S
-
|
Apalutamide D4
ARN-509 D4
|
Androgen Receptor
|
Cancer
|
|
Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
|
-
- HY-103090
-
-
- HY-117965
-
-
- HY-P0097A
-
-
- 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-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-15770
-
-
- HY-B1107
-
|
Naftidrofuryl oxalate
Nafronyl oxalate salt
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.
|
-
- HY-16681
-
|
AGN 194310
VTP-194310
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively.
|
-
- HY-129059
-
|
Odapipam
NNC 756
|
Dopamine Receptor
|
Neurological Disease
|
|
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer.
|
-
- HY-107568
-
-
- HY-119093
-
-
- HY-100806
-
-
- HY-B0745
-
-
- HY-100783
-
|
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-108908
-
-
- HY-10301
-
|
MK-3207
|
CGRP Receptor
|
Neurological Disease
|
|
MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
|
-
- HY-107512
-
-
- HY-135230
-
|
LY2444296
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
|
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
|
-
- HY-B0115A
-
-
- HY-P1233A
-
-
- HY-A0008
-
-
- HY-19344
-
|
Lifitegrast
SAR 1118; SHP-606
|
Integrin
|
Inflammation/Immunology
|
|
Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
|
-
- HY-101213
-
|
OSW-1
|
Others
|
Cancer
|
|
OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
|
-
- HY-19529
-
-
- HY-136255
-
|
AZD-9833
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD-9833 is a potent and orally active estrogen receptor (ER) antagonist. AZD-9833 is used for the study of
ER + HER2-advanced breast cancer.
|
-
- HY-B0002A
-
|
Ondansetron hydrochloride dihydrate
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-103090A
-
-
- HY-135270
-
-
- HY-N0584A
-
|
Anisodamine hydrobromide
6-Hydroxyhyoscyamine hydrobromide
|
mAChR
|
Inflammation/Immunology
|
|
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties.
|
-
- HY-115066
-
-
- HY-17369
-
-
- HY-15454
-
|
Xevinapant
AT-406; Debio 1143; SM-406
|
IAP
|
Cancer
|
|
Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
|
-
- HY-115066A
-
-
- HY-107051
-
-
- HY-B0437AS
-
-
- HY-16780
-
-
- HY-111308
-
-
- HY-17572
-
|
Atosiban
RW22164; RWJ22164
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
|
-
- HY-105124A
-
-
- HY-P1471
-
-
- HY-12790
-
-
- HY-14136
-
-
- HY-15472
-
-
- HY-15069A
-
|
Fanapanel hydrate
ZK200775 (hydrate); MPQX hydrate
|
iGluR
|
Neurological Disease
|
|
Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-P0205B
-
-
- HY-14137
-
-
- HY-B1205
-
|
Atropine
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Neurological Disease
|
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist, with anti-myopia effect. Atropine blocks the inhibitory effect of ACh on heart rate and contractility, potentially also leading to tachyarrhythmias.
|
-
- 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-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-A0118
-
|
Naloxegol
NKTR-118; AZ-13337019
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
|
-
- HY-15744
-
-
- HY-B0532S
-
-
- HY-14777
-
|
Radiprodil
RGH-896
|
iGluR
|
Neurological Disease
|
|
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
|
-
- HY-101731
-
-
- HY-108677
-
|
L-368,899 hydrochloride
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.
|
-
- HY-N6969
-
|
Dicentrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates.
|
-
- HY-30234A
-
-
- HY-B1281
-
-
- HY-P1263
-
-
- HY-100483
-
|
A-804598
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-B1621A
-
|
Cyclopentolate hydrochloride
DL-Cyclopentolate hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice.
|
-
- HY-106441A
-
|
Rislenemdaz
MK-0657; CERC-301
|
iGluR
|
Neurological Disease
|
|
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
|
-
- HY-15069
-
|
Fanapanel
ZK200775; MPQX
|
iGluR
|
Neurological Disease
|
|
Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-15084A
-
|
(-)-Dizocilpine maleate
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
|
-
- HY-N4225
-
-
- HY-136146
-
|
SUVN-911
|
nAChR
|
Neurological Disease
|
|
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
|
-
- HY-10095A
-
|
Olcegepant hydrochloride
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
|
-
- HY-108908A
-
|
Modipafant
UK-80067
|
Others
|
Inflammation/Immunology
|
|
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
|
-
- HY-133113
-
-
- 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-70050B
-
-
- HY-U00399
-
-
- HY-10792A
-
-
- HY-15370A
-
-
