Search Result
Results for "Antifolate Antagonists" in MCE Product Catalog:
1720
Inhibitors & Agonists
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- 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-50159
-
-
- HY-50158
-
-
- HY-50713
-
-
- HY-130569
-
|
7-Hydroxymethotrexate
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- 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-19947
-
|
PF-06291874
Glucagon receptor Antagonists-4
|
Glucagon Receptor
|
Metabolic Disease
|
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
|
-
- 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. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- 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. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- 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.
|
-
- HY-137773
-
|
N-Methyl pemetrexed
|
Others
|
Cancer
|
|
N-Methyl pemetrexed is an impurity of Pemetrexed. Pemetrexed is an antifolate cytotoxic agent that can be used for the research of cancer.
|
-
- HY-110303
-
-
- 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.
|
-
- HY-133533
-
-
- HY-133112
-
-
- HY-100382
-
|
FPTQ
|
mGluR
|
Others
|
|
FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
|
-
- HY-135147
-
|
ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-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.
|
-
- HY-14407
-
-
- 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.
|
-
- HY-16474
-
|
Relugolix
TAK-385
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
|
-
- HY-133887
-
-
- HY-133624
-
|
1,1,3-Tribromoacetone
|
Others
|
Cancer
|
|
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- HY-14407A
-
-
- 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.
|
-
- 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-129441
-
-
- HY-N6932
-
-
- 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-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).
|
-
- 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.
|
-
- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
Apoptosis
|
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.
|
-
- HY-101283
-
|
HCH6-1
|
Others
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
|
-
- HY-111500
-
-
- 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.
|
-
- HY-P1185A
-
-
- HY-112562
-
-
- HY-112265
-
-
- HY-18075
-
-
- HY-112264
-
-
- HY-101264
-
-
- HY-22437
-
-
- HY-U00334
-
-
- HY-118844
-
-
- HY-U00375
-
-
- HY-U00320
-
-
- HY-U00121
-
-
- HY-U00330
-
-
- HY-B1439B
-
-
- HY-B0918
-
-
- HY-107430
-
|
Oxythiamine
Hydroxythiamin
|
Others
|
Cancer
|
|
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
|
-
- HY-110037
-
-
- HY-136922
-
-
- HY-U00331
-
-
- HY-129995
-
|
TSHR antagonist S37b
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
|
-
- HY-101704
-
-
- HY-112792
-
-
- HY-U00408
-
-
- HY-B1205A
-
|
Atropine sulfate
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist.
|
-
- HY-117793
-
-
- HY-100321
-
-
- HY-U00359
-
-
- HY-15257A
-
-
- HY-137175
-
|
TMBIM6 antagonist-1
|
mTOR
|
Cancer
|
|
TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+.
|
-
- HY-B0548S1
-
-
- HY-U00360
-
-
- HY-121186
-
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- HY-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-112430
-
-
- HY-117153
-
-
- HY-111484
-
-
- HY-70002B
-
-
- HY-N1163
-
-
- 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.
|
-
- HY-114193
-
-
- HY-114194
-
-
- HY-U00368
-
-
- HY-15540
-
-
- HY-B2111
-
-
- HY-110203
-
|
R-7050
TNF-α Antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- 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).
|
-
- HY-137093
-
-
- HY-100648
-
-
- HY-100649
-
-
- HY-129357
-
-
- HY-100248
-
-
- HY-Z0816
-
-
- HY-U00067
-
-
- HY-101685
-
-
- HY-111669
-
-
- HY-124759
-
-
- HY-111443
-
-
- 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-U00286
-
-
- HY-112056
-
-
- HY-15277
-
-
- HY-101638
-
-
- 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.
|
-
- HY-16991
-
-
- HY-B1547A
-
-
- HY-100266
-
-
- HY-19223
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-U00017
-
-
- HY-129946
-
-
- HY-B0524A
-
-
- HY-U00365
-
-
- HY-131449
-
-
- HY-D0237
-
-
- HY-B0524
-
-
- HY-U00397
-
-
- HY-12503
-
-
- HY-12195
-
-
- HY-125820
-
-
- 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.
|
-
- HY-19818A
-
-
- HY-U00321
-
-
- HY-19705B
-
-
- HY-N2189
-
-
- HY-120588
-
-
- HY-109139
-
-
- HY-13242
-
|
Taladegib
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
-
- HY-15372
-
-
- HY-106910
-
-
- HY-100850
-
-
- HY-B1589A
-
-
- HY-B1014
-
-
- HY-101574
-
-
- HY-101594
-
-
- HY-U00062
-
-
- HY-101675
-
-
- HY-101707
-
-
- HY-B1240
-
-
- HY-105117
-
-
- HY-102024
-
-
- HY-16346S
-
-
- HY-128878
-
-
- HY-U00322
-
-
- HY-17039S
-
-
- HY-G0014B
-
-
- HY-G0014A
-
-
- HY-111449
-
-
- HY-130992
-
-
- HY-101534
-
-
- HY-U00247
-
-
- HY-B0768A
-
-
- HY-U00245
-
-
- HY-13202
-
-
- HY-U00202
-
-
- HY-B0460
-
-
- HY-100173
-
-
- HY-100903
-
-
- HY-N0219
-
-
- HY-B1165
-
-
- HY-B0462A
-
-
- HY-U00110
-
-
- HY-103531
-
-
- HY-B0325
-
-
- HY-16635
-
-
- HY-U00119
-
-
- HY-101691
-
-
- HY-B0547A
-
-
- HY-B1303A
-
-
- HY-13209
-
-
- HY-B2154
-
-
- HY-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-B0561
-
-
- HY-116649
-
-
- HY-131256
-
-
- HY-P1025
-
-
- HY-N2079
-
-
- HY-N6628
-
-
- HY-U00234
-
-
- HY-A0027
-
-
- HY-100255
-
-
- HY-110110
-
-
- HY-U00139
-
-
- HY-A0250
-
-
- HY-100454
-
-
- HY-112620
-
-
- HY-B0205
-
-
- HY-B1283
-
-
- HY-B1303
-
-
- HY-100292
-
-
- HY-15539
-
-
- HY-101745
-
-
- HY-101743
-
-
- HY-B0286A
-
-
- HY-B1164
-
-
- HY-17465
-
-
- HY-P1329
-
-
- HY-100191
-
-
- HY-112248
-
-
- HY-19733
-
-
- 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-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-14778
-
-
- HY-16168A
-
-
- HY-15085
-
-
- HY-17037
-
-
- HY-B2168
-
-
- HY-19732
-
-
- HY-16763
-
-
- HY-B0009
-
-
- HY-P1329A
-
-
- HY-10164
-
-
- HY-101632
-
-
- HY-U00019
-
-
- HY-101600
-
-
- HY-101618
-
-
- HY-15073
-
-
- HY-B0895
-
-
- HY-18555
-
|
TMPA
|
Others
|
Others
|
|
TMPA is an antagonist of nuclear receptor Nur77 and LKB1 interaction.
|
-
- HY-18101A
-
-
- HY-U00040
-
-
- 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-102037
-
-
- HY-133123
-
-
- HY-125821
-
|
Sigma-1 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
|
-
- HY-102004
-
-
- HY-42849
-
-
- HY-13021
-
-
- HY-17582
-
-
- HY-15001
-
-
- HY-100471
-
-
- HY-19737A
-
-
- HY-101502A
-
-
- HY-12710A
-
-
- HY-16509
-
-
- HY-112703
-
-
- HY-14538A
-
-
- HY-P0061
-
-
- HY-13439
-
-
- HY-50663
-
-
- HY-42849A
-
-
- HY-101797
-
-
- HY-A0066
-
-
- HY-15758
-
-
- HY-U00018
-
-
- HY-19243
-
-
- HY-101668
-
-
- HY-15105
-
-
- HY-101679
-
-
- HY-19163
-
-
- HY-103099
-
-
- HY-100153
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-14538
-
-
- HY-N0096
-
-
- HY-114191A
-
-
- HY-101116
-
-
- HY-125819
-
-
- HY-B1416A
-
-
- HY-103213
-
-
- 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-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
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-N0607
-
-
- HY-100637
-
|
Hydroxybupropion
|
Adrenergic Receptor
nAChR
|
Neurological Disease
|
|
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .
|
-
- HY-A0066A
-
-
- HY-17492
-
-
- HY-B0774
-
-
- HY-76520
-
-
- HY-15709
-
-
- HY-110095
-
-
- HY-18697
-
-
- HY-15574
-
-
- HY-19768
-
-
- HY-102093
-
-
- HY-12426
-
-
- HY-12380
-
-
- HY-B1487
-
-
- HY-B0004
-
-
- HY-12380A
-
-
- HY-16732
-
-
- HY-U00363
-
-
- HY-A0075
-
-
- 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-B2073A
-
-
- HY-16701
-
|
BV6
|
IAP
|
Cancer
|
|
BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
|
-
- HY-12510
-
-
- HY-15574A
-
-
- HY-P0264
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-B2073
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-101706
-
-
- HY-101830
-
-
- HY-101721
-
-
- HY-50912
-
-
- HY-P0209
-
-
- HY-U00283
-
-
- HY-15702
-
|
HJC0350
|
Others
|
Cancer
|
|
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
|
-
- HY-U00404
-
-
- HY-U00188
-
-
- HY-U00207
-
-
- HY-50691
-
-
- 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-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-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-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
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-100607A
-
-
- HY-U00443
-
-
- HY-B1438
-
-
- HY-112667
-
-
- HY-U00263
-
-
- HY-B0682A
-
-
- HY-B0355
-
-
- HY-101527
-
|
20-HEDE
WIT 002
|
Others
|
Cancer
|
|
20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
|
-
- HY-10259
-
-
- HY-16692
-
-
- HY-15108
-
-
- HY-112050
-
-
- HY-110110A
-
-
- HY-13541
-
|
ADH-1
|
Others
|
Cancer
|
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-14423
-
-
- HY-A0033
-
-
- HY-B0500
-
-
- HY-B0298A
-
-
- HY-B1108
-
-
- HY-U00212
-
-
- HY-101177
-
-
- HY-11103
-
-
- HY-14369
-
-
- HY-18611A
-
-
- HY-107765
-
-
- HY-108324
-
-
- HY-10259A
-
-
- HY-14130
-
-
- HY-N1378
-
-
- HY-14447
-
-
- HY-18611
-
-
- HY-101683
-
-
- HY-14129
-
-
- HY-19855
-
-
- HY-15853
-
-
- HY-15640
-
-
- HY-13004
-
-
- HY-13796
-
-
- HY-118861A
-
-
- HY-103533
-
-
- HY-14432
-
-
- HY-101407
-
-
- HY-14277A
-
-
- HY-105201
-
|
Fabesetron
FK1052 free base
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
|
-
- HY-B0569
-
|
Hexamethonium Bromide
|
nAChR
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.
|
-
- 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-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-B0781
-
-
- 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-103200
-
-
- HY-100672
-
-
- HY-112558
-
-
- HY-13541A
-
-
- HY-N0184
-
-
- HY-B0192A
-
-
- HY-P0171
-
-
- HY-W014325
-
-
- HY-B0192
-
-
- HY-50669A
-
-
- HY-15412
-
|
HhAntag
|
Smo
|
Cancer
|
|
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
|
-
- 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-10560
-
-
- HY-12635
-
-
- HY-U00253
-
-
- HY-U00106
-
-
- HY-19632
-
-
- HY-B0549A
-
-
- HY-19193
-
-
- HY-100152
-
-
- HY-110136A
-
-
- HY-19391
-
-
- 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-10052
-
-
- HY-19914
-
-
- HY-U00252
-
-
- HY-B0369A
-
-
- HY-B0412
-
-
- HY-12752A
-
-
- HY-43711
-
-
- HY-B1510
-
-
- HY-17001A
-
-
- HY-19654
-
-
- HY-101620
-
-
- HY-101700
-
-
- HY-101669
-
-
- HY-17505
-
-
- HY-B1225
-
-
- HY-101718
-
-
- HY-14538S1
-
-
- HY-108997
-
-
- HY-B1613A
-
-
- HY-15319B
-
-
- 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-116637
-
|
Tetrahydromagnolol
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
|
-
- HY-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-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-32329A
-
|
Setiptiline maleate
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
|
Setiptiline (MO-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-107743
-
|
Naloxone benzoylhydrazone
NalBzoH
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.
|
-
- HY-100703
-
-
- HY-16978
-
-
- HY-112629
-
-
- HY-17001
-
-
- HY-B0538A
-
-
- HY-A0012
-
-
- HY-B1517A
-
-
- HY-P1558
-
-
- HY-17512
-
-
- HY-15195
-
-
- HY-W018061
-
-
- HY-B1081
-
-
- HY-12426A
-
-
- HY-13059B
-
-
- HY-U00356
-
-
- HY-15462
-
-
- HY-U00392
-
-
- HY-B0539
-
-
- HY-19057A
-
-
- HY-B1435
-
-
- HY-13059
-
-
- HY-B0716
-
-
- HY-18966
-
-
- HY-15411
-
-
- HY-10634
-
-
- HY-U00251
-
-
- HY-18204
-
-
- HY-12799
-
-
- HY-B1517
-
-
- 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-U00084
-
-
- HY-19909
-
|
NRC-2694
|
EGFR
|
Cancer
|
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-19110
-
-
- HY-U00076
-
-
- HY-19274
-
-
- HY-111398
-
-
- HY-U00105
-
-
- HY-15541
-
-
- HY-12377
-
-
- HY-B0909
-
-
- HY-10064
-
-
- HY-14751
-
-
- HY-B1126
-
-
- HY-100308
-
-
- HY-A0295
-
-
- 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-15403
-
-
- HY-50901
-
-
- 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) is the R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-13059A
-
-
- HY-B0431A
-
-
- HY-B0478
-
-
- HY-10995
-
-
- HY-19347
-
-
- HY-P1014
-
-
- HY-114025
-
-
- HY-13534
-
-
- HY-108688
-
-
- HY-A0021
-
-
- HY-14338A
-
-
- HY-100882
-
-
- HY-A0018
-
-
- HY-120090
-
-
- 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-101105A
-
-
- HY-B0202
-
-
- HY-10486
-
-
- HY-14914
-
-
- HY-B0780
-
-
- HY-17024
-
-
- HY-12428
-
-
- HY-19191
-
-
- HY-12131
-
-
- HY-14938
-
-
- HY-19025
-
-
- HY-19969
-
-
- HY-118678
-
-
- 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) is the S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-U00143
-
-
- HY-N0145
-
-
- HY-12777
-
-
- HY-U00354
-
-
- HY-12301
-
-
- HY-N2332A
-
-
- HY-12715
-
-
- 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-101755
-
-
- HY-15084
-
-
- HY-P1017
-
-
- HY-16993
-
-
- HY-15009
-
-
- HY-50175
-
-
- HY-108251
-
-
- HY-100717
-
-
- HY-15577
-
|
GSK3787
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- 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-15068
-
|
NBQX
FG9202
|
iGluR
|
Neurological Disease
|
|
NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
|
-
- HY-19736
-
-
- HY-B1059
-
-
- HY-16023A
-
-
- HY-B0595
-
-
- HY-W040146
-
-
- HY-15403A
-
-
- HY-B0661A
-
-
- HY-A0163
-
-
- HY-B0205S
-
-
- HY-B0325S
-
-
- 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-U00402
-
-
- HY-19097
-
-
- HY-U00077
-
-
- HY-19048
-
-
- HY-U00028
-
-
- HY-U00237
-
-
- HY-B1305
-
-
- HY-101022
-
-
- HY-B0354A
-
-
- HY-P0061A
-
-
- HY-14249
-
-
- HY-15538
-
-
- HY-N4247
-
-
- HY-B1081A
-
-
- HY-B0394
-
-
- HY-101986
-
-
- 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-101586
-
-
- 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-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-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-12488
-
-
- HY-15726
-
-
- HY-B0686
-
-
- HY-15851
-
-
- HY-12940
-
-
- HY-P0009B
-
-
- 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-10900
-
-
- HY-P0009A
-
-
- HY-17390
-
-
- HY-U00137
-
-
- HY-109593
-
-
- HY-104020A
-
-
- HY-16060
-
-
- HY-110255
-
-
- HY-B0686A
-
-
- HY-A0013A
-
-
- 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-101686
-
-
- HY-107437
-
-
- HY-A0013
-
-
- HY-110255A
-
-
- HY-10888
-
-
- HY-17390A
-
-
- HY-15481
-
-
- 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-P1309A
-
-
- 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-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-B0674
-
-
- HY-107735
-
-
- HY-17428
-
-
- HY-50081
-
-
- HY-13677
-
-
- HY-109002
-
-
- 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-70002
-
-
- HY-119217
-
-
- 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-12780S
-
-
- HY-17000
-
-
- 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-15488
-
-
- HY-B0303A
-
-
- HY-101844
-
-
- HY-15653
-
-
- HY-19900
-
-
- HY-B0071A
-
-
- HY-10487
-
-
- 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-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-101727
-
-
- HY-12127
-
-
- HY-116408A
-
-
- HY-17351
-
-
- HY-101953
-
-
- HY-105545
-
|
Dexetimide
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
|
mAChR
|
Neurological 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-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-A0125A
-
-
- HY-18263C
-
|
Elubrixin tosylate
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
|
-
- 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-101910
-
-
- HY-15443
-
-
- HY-15676
-
-
- HY-P1276
-
-
- HY-P0216
-
-
- HY-15370
-
-
- HY-10857
-
-
- HY-17004
-
-
- 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-113534
-
|
MV1
|
IAP
Apoptosis
|
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-12366
-
-
- HY-17436
-
-
- HY-103361
-
-
- 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-13535A
-
-
- HY-B0377
-
-
- HY-101809
-
-
- HY-101815
-
-
- HY-19477
-
-
- HY-19189
-
-
- HY-19062
-
-
- HY-15068A
-
|
NBQX disodium
FG9202 disodium
|
iGluR
|
Neurological Disease
|
|
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
|
-
- HY-103456
-
-
- HY-13508
-
-
- 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-101458A
-
-
- HY-U00238
-
-
- HY-B1494
-
-
- HY-15799
-
-
- 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-B0031S
-
-
- HY-14791A
-
-
- HY-100720
-
-
- HY-N0127
-
-
- HY-12525
-
-
- HY-B0750B
-
-
- HY-15421
-
-
- HY-U00185
-
-
- HY-12765S
-
-
- 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-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-17512A
-
-
- HY-17621
-
-
- HY-100129
-
-
- HY-19205A
-
-
- HY-10792
-
-
- HY-B0750A
-
-
- HY-101179
-
-
- 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-P1203
-
-
- HY-U00151
-
-
- HY-P1727
-
|
Super-TDU
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.
|
-
- HY-103449
-
-
- HY-101619
-
-
- 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-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-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-13274
-
-
- HY-12497
-
-
- HY-128379
-
|
Labetalone hydrochloride
|
Others
|
Others
|
|
Labetalone hydrochloride is an impurity of Labetalol. Labetalol is an orally active adrenoceptor blocking drug which is a competitive antagonist at both alpha- and beta-adrenoceptor sites.
|
-
- HY-10633
-
-
- 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-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-P2542
-
-
- HY-P1869
-
-
- HY-13505
-
-
- HY-I0230
-
-
- HY-14736
-
-
- HY-16040
-
-
- HY-19989A
-
-
- 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-P1203A
-
-
- HY-10794
-
-
- HY-B0164A
-
-
- HY-101924
-
-
- HY-17410A
-
-
- HY-107382
-
-
- HY-13466
-
-
- HY-U00355
-
-
- HY-10011
-
-
- HY-16711
-
-
- HY-B0115
-
-
- HY-101430
-
-
- 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-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-10889
-
-
- HY-136462
-
|
CYM50358
|
LPL Receptor
|
Infection
|
|
CYM50358 is a potent and selective S1PR4 antagonist, with an IC50 of 25 nM. CYM50358 can be used for the research of influenza infection.
|
-
- HY-B0164
-
-
- 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-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-30152
-
-
- 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-100562
-
-
- HY-B1541
-
-
- HY-13683
-
-
- HY-12142
-
-
- HY-131914A
-
-
- 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-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-U00072
-
-
- 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-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-119802
-
-
- HY-107382A
-
-
- HY-17410
-
-
- 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-13222
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-116790A
-
-
- HY-B1789A
-
-
- 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-P1276A
-
-
- HY-15708
-
-
- 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-10388A
-
-
- HY-15418
-
-
- 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-19904
-
-
- 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-75766S
-
-
- HY-15834A
-
-
- 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-103088
-
-
- HY-U00433A
-
-
- 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-14880B
-
-
- HY-103454
-
-
- 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-19532
-
-
- HY-14537
-
-
- HY-12336
-
-
- HY-12981
-
-
- HY-P1233
-
-
- HY-B1552B
-
-
- 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-131041
-
|
Ned-K
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes.
|
-
- HY-18347A
-
-
- HY-120261
-
-
- HY-14339
-
-
- HY-13245
-
-
- 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-17446
-
-
- HY-U00117
-
-
- HY-10871
-
-
- 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-11029
-
-
- HY-108896
-
-
- 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-133555
-
-
- HY-B0407A
-
-
- HY-17369
-
-
- 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-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- 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-17497A
-
-
- HY-135589
-
-
- HY-B0031S1
-
-
- HY-15950
-
-
- HY-108329
-
-
- 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-112302
-
-
- HY-14875
-
-
- HY-13527
-
-
- HY-14545A
-
-
- HY-131276
-
-
- HY-14121
-
-
- 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-16996A
-
-
- HY-17497S
-
-
- HY-10013A
-
-
- 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-107723
-
-
- 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-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-A0002
-
-
- 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-14914S
-
|
Azilsartan D5
TAK-536 D5
|
Angiotensin Receptor
|
Others
|
|
Azilsartan D5 (TAK-536 D5) is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
|
-
- HY-12294A
-
-
- HY-120691A
-
-
- HY-B0548S
-
-
- HY-14545
-
-
- HY-B0115A
-
-
- 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-B0323
-
-
- 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-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-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-B0437
-
-
- HY-N0079
-
-
- HY-N6066
-
-
- HY-B0548AS
-
-
- HY-100316
-
-
- HY-17617
-
-
- HY-131255
-
-
- 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-50697
-
-
- HY-A0081
-
-
- HY-B0801A
-
-
- 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-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-12005
-
-
- 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-105542
-
-
- HY-P1479
-
-
- HY-N0471
-
|
L-Hyoscyamine
Daturine
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
|
-
- 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-101106
-
|
AR7
|
RAR/RXR
|
Cancer
Neurological Disease
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- 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-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-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-14825A
-
-
- HY-I0021
-
-
- HY-B1486
-
-
- HY-12190
-
-
- HY-P1233A
-
-
- HY-17004S
-
|
Olmesartan D4
RNH-6270 D4
|
Angiotensin Receptor
|
Others
|
|
Olmesartan D4 (RNH-6270 D4) is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
|
-
- HY-Y0313
-
-
- HY-10806
-
-
- HY-15894
-
-
- 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-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-P1479A
-
-
- HY-133775
-
-
- 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-12100
-
-
- HY-10562
-
-
- 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-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-B1505
-
-
- HY-107051
-
-
- HY-101690
-
-
- HY-101348
-
-
- HY-13955
-
-
- 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-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-12790
-
-
- HY-10805A
-
-
- 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-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-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-131942
-
-
- HY-P0205B
-
-
- 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-108250
-
|
(R)-Bicalutamide
|
Androgen Receptor
|
Cancer
|
|
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
|
-
- HY-17512S
-
-
- HY-B0068
-
-
- 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-10898
-
-
- HY-B0745
-
-
- HY-B1270
-
-
- HY-10805
-
-
- 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-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-B0716S
-
-
- HY-15043
-
-
- HY-100183
-
-
- HY-104003
-
-
- HY-B0365A
-
-
- HY-P3066
-
|
SKF 100398
d(CH2)5Tyr(Et)VAVP
|
Vasopressin Receptor
|
Metabolic Disease
|
|
SKF 100398 (d(CH2)5Tyr(Et)VAVP) is an arginine vasopressin (AVP) analogue, and acts as a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
|
-
- 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-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-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-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-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-B0462
-
-
- 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-10302
-
-
- 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-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-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-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-103090
-
-
- 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-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-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-15472
-
-
- HY-B0321
-
|
Tropicamide
Ro 1-7683
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops.
|
-
- HY-U00367
-
-
- HY-A0015
-
-
- 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-B0366A
-
-
- HY-15744
-
-
- HY-100806
-
-
- 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-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-101385
-
-
- HY-101784
-
-
- 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-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-13713
-
-
- HY-18689
-
|
SYM2206
|
iGluR
|
Neurological Disease
|
|
SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC50 of 1.6 μM. SYM2206 blocks Nav1.6-mediated persistent currents.
|
-
- 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-124543
-
-
- 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-14185
-
-
- HY-115066A
-
-
- 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-P2497
-
-
- HY-B1808A
-
-
- HY-123918
-
|
JMS-17-2
|
Others
|
Cancer
Endocrinology
|
|
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells.
|
-
- HY-16935
-
|
Mavatrep
JNJ-39439335
|
TRP Channel
|
Others
|
|
Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
|
-
- HY-N4225
-
-
- HY-11021
-
|
Elinogrel
PRT060128
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects.
|
-
- HY-B0437AS
-
-
- HY-16780
-
-
- 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-117606
-
|
LY3027788
|
mGluR
|
Neurological Disease
|
|
LY3027788, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 has antidepressant efficacy.
|
-
- 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-17369B
-
|
Tirofiban
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
Target: integrin IIb/IIIa
Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
|
-
- HY-B0411
-
|
Domperidone
R33812
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
|
-
- HY-133113
-
-
- HY-N0471A
-
|
L-Hyoscyamine sulfate
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205).
|
-
- HY-13408
-
|
(+)-Apogossypol
Apogossypol; NSC736630
|
Bcl-2 Family
|
Cancer
|
|
(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.
|
-
- 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-11063
-
-
- 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-B0548
-
-
- HY-119093
-
-
- 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. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-135387
-
-
- HY-B1470
-
|
Azaperone
R-1929
|
Dopamine Receptor
|
Neurological Disease
|
|
Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
|
-
- HY-101731
-
-
- HY-123918A
-
-
- HY-107633
-
|
A 1120
|
Others
|
Metabolic Disease
|
|
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.
|
-
- 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-A0008
-
-
- HY-B1301
-
-
- HY-14184
-
-
- 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-B0140
-
-
- HY-109024
-
-
- HY-135270
-
-
- HY-136338
-
|
Cimetidine sulfoxide
Cimetidine sulphoxide
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment.
|
-
- HY-13738A
-
|
Raloxifene hydrochloride
Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
|
-
- HY-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-B1019
-
|
Sulpiride
|
Dopamine Receptor
|
Neurological Disease
|
|
Sulpiride is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class, used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression.
|
-
- HY-12707
-
-
- HY-B0160
-
-
- HY-13575S1
-
-
- 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-P1471
-
-
- HY-112596A
-
-
- HY-133111
-
-
- HY-114244
-
|
USL311
|
CXCR
|
Cancer
Endocrinology
|
|
USL311 is a selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
|
-
- HY-19168
-
|
Perzinfotel
EAA-090
|
iGluR
|
Neurological Disease
|
|
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site.
|
-
- HY-14136
-
-
- HY-14882A
-
-
- HY-P0097A
-
-
- HY-15067
-
|
DNQX
FG 9041
|
iGluR
|
Cancer
|
|
DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively).
|
-
- HY-B0461
-
|
Trospium chloride
|
mAChR
|
Neurological Disease
|
|
Trospium chloride is a specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors.
|
-
- HY-13575S
-
-
- 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-18006
-
-
- HY-P2319
-
-
- HY-14137
-
-
- 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-126136
-
|
ML303
|
Influenza Virus
|
Infection
|
|
ML303 is a pyrazolopyridine influenza virus nonstructural protein 1 (NS1) antagonist (IC90 = 155 nM), with an EC50 of 0.7 μM for Influenza A virus H1N1.
|
-
- 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-10792A
-
-
- HY-10562A
-
-
- HY-15370A
-
-
- HY-112596
-
|
H3B-6545
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
|
-
- HY-10095
-
|
Olcegepant
BIBN-4096; BIBN 4096BS
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
|
-
- HY-17572A
-
|
Atosiban acetate
RW22164 acetate; RWJ22164 acetate
|
Oxytocin Receptor
Vasopressin Receptor
|
Cancer
Endocrinology
|
|
Atosiban acetate (RW22164 acetate;RWJ22164 acetate) 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-P1277
-
-
- HY-103568
-
|
YM-298198 hydrochloride
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
|
-
- HY-13848
-
-
- HY-13951
-
-
- HY-B1281
-
-
- HY-P1263
-
-
- HY-19529
-
-
- HY-15722
-
-
- HY-11100
-
|
Asenapine maleate
Org 5222 maleate
|
5-HT Receptor
|
Neurological Disease
|
|
Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
|
-
- 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-13696
-
-
- 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-P1277A
-
-
- 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-14184A
-
-
- HY-108912
-
-
- HY-111444
-
|
Auxinole
|
Others
|
Others
|
|
Auxinole is a potent auxin antagonist of TIR1/AFB receptors, binding TIR1 to block the formation of the TIR1-IAA-Aux/IAA complex and so inhibits auxin-responsive gene expression.
|
-
- HY-106628
-
|
Sudoxicam
|
COX
|
Inflammation/Immunology
|
|
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.
|
-
- HY-P2319A
-
-
- HY-B0743A
-
|
Pipecuronium bromide
|
nAChR
|
Neurological Disease
|
|
Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM.
|
-
- HY-131289
-
|
LY3020371
|
mGluR
|
Neurological Disease
|
|
LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression.
|
-
- HY-12080
-
|
BX471
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-100714A
-
|
D-AP5
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
|
-
- HY-16725
-
-
- HY-B0548A
-
-
- HY-12025
-
|
Serdemetan
JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
|
-
- HY-108539
-
|
CE3F4
|
Others
|
Cardiovascular Disease
|
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-W011955
-
-
- HY-13738
-
|
Raloxifene
Keoxifene; LY156758 free base; LY139481
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
|
-
- HY-14289
-
|
Cimetidine
SKF-92334
|
Histamine Receptor
|
Cancer
Endocrinology
|
|
Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.
|
-
- HY-B1317
-
|
Thonzylamine
Neohetramine
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases.
|
-
- HY-101622
-
-
- HY-15320
-
-
- HY-B1395
-
|
Mecamylamine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.
|
-
- HY-12080A
-
-
- HY-10053
-
|
Maropitant
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
|
-
- HY-B0274
-
-
- HY-P1263A
-
-
- HY-121018
-
|
Daltroban
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
|
-
- HY-B0305A
-
|
Roxatidine Acetate Hydrochloride
HOE 760
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Roxatidine Acetate Hydrochloride (HOE 760) is a selective histamine H2 receptor antagonist, can be used for the research of gastric and duodenal ulcers. Roxatidine Acetate Hydrochloride can be rapidly converted to its active metabolite, roxatidine, by esterases in the small intestine, plasma, and liver.
|
-
- HY-110237
-
|
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-16039
-
|
AM095
|
LPL Receptor
|
Inflammation/Immunology
|
|
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
|
-
- HY-15450A
-
|
INCB 3284
|
CCR
|
Endocrinology
|
|
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
|
-
- HY-B1238
-
|
Pronethalol
(±)-Pronethalo
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
|
-
- HY-114412A
-
-
- HY-135829
-
|
BAY 2416964
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
|
-
- HY-15989A
-
|
SM-164 Hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- HY-B0274A
-
-
- HY-B0128
-
|
Diphylline
Diprophylline
|
Adenosine Receptor
Phosphodiesterase (PDE)
|
Infection
|
|
Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator drug and has the potential for chronic bronchitis and emphysema.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-116213
-
-
- HY-U00399
-
-
- HY-15731
-
-
- HY-17450
-
|
Aplaviroc
AK 602; GSK 873140; GW 873140
|
CCR
HIV
|
Infection
Endocrinology
|
|
Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
|
-
- HY-70068
-
-
- HY-14406A
-
-
- HY-14609
-
|
MPEP Hydrochloride
|
mGluR
|
Neurological Disease
|
|
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects.
|
-
- HY-B1238A
-
-
- HY-12600
-
|
AZD5582
|
IAP
Apoptosis
|
Cancer
|
|
AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
|
-
- HY-B0358A
-
-
- HY-109095
-
-
- HY-15445
-
|
CTEP
RO 4956371; mGluR5 inhibitor
|
mGluR
|
Neurological Disease
|
|
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
|
-
- HY-114379
-
|
AS2717638
|
LPL Receptor
|
Inflammation/Immunology
|
|
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia.
|
-
- HY-14609A
-
|
MPEP
|
mGluR
|
Neurological Disease
|
|
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects.
|
-
- HY-112051
-
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.
|
-
- HY-101946
-
|
AS-35
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
|
-
- HY-16346
-
-
- HY-15989
-
|
SM-164
|
IAP
Apoptosis
|
Cancer
|
|
SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- 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-N0301
-
|
Thiocolchicoside
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
|
-
- HY-135303
-
|
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-15517B
-
|
KN-92 hydrochloride
|
Others
|
Cancer
|
|
KN-92 hydrochloride is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 hydrochloride is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93.
|
-
- HY-B0982
-
-
- HY-B1371A
-
-
- HY-18971
-
-
- HY-136208
-
|
TAN-452
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
|
-
- HY-100937
-
|
DPCPX
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
|
-
- HY-P1050
-
|
COG 133
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM.
|
-
- HY-15895
-
-
- HY-117508
-
-
- HY-B1693
-
|
Levomepromazine
Methotrimeprazine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Levomepromazine (Methotrimeprazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors.
|
-
- HY-118561
-
|
Bermoprofen
AD-1590
|
Others
|
Inflammation/Immunology
|
|
Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory agent. Bermoprofen has potent antipyretic and analgesic activities with a short biological half-life. Bermoprofen is a potent antagonist of LPS-induced fever in rabbits.
|
-
- HY-14153A
-
-
- HY-106139
-
|
Bimosiamose
TBC-1269
|
Others
|
Inflammation/Immunology
|
|
Bimosiamose (TBC-1269) is a nonoligosaccharide pan-selectin antagonist with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose has anti-inflammatory effects.
|
-
- HY-15071
-
|
YM90K
|
iGluR
|
Neurological Disease
|
|
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions.
|
-
- HY-19889
-
-
- HY-100301
-
-
- HY-136142
-
|
Prasugrel chloride impurity
|
Others
|
Others
|
|
Prasugrel chloride impurity is a catp impurity of Prasugrel, exacted from patent US20130345428A1, line 0053. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-11083
-
|
GW-803430
GW-3430
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity.
|
-
- HY-15319
-
-
- HY-16687A
-
-
- HY-P1201
-
|
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-N2510
-
|
Myristicin
Myristicine
|
5-HT Receptor
|
Neurological Disease
|
|
Myristicine act as a serotonin receptor antagonist, a weak monamine oxidase (MAO) inhibitor. Myristicine is the main component of nutmeg essential oil from Myristica fragrans Houtt. Myristicine abuse produce hallucinogenic effects, organ damage, deliriumand others.
|
-
- HY-125901
-
|
D-Tubocurarine chloride pentahydrate
|
nAChR
|
Neurological Disease
|
|
D-Tubocurarine chloride pentahydrate is the chloride salt form of Tubocurarine, a nicotinic acetylcholine receptors (AChR) antagonist, and can be used as a skeletal muscle relaxant during surgery or mechanical ventilation. D-Tubocurarine chloride pentahydrate is also a potent neuromuscular blocking agent.
|
-
- HY-10858
-
|
WAY 316606
|
sFRP-1
|
Cancer
|
|
WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
|
-
- HY-19337
-
|
ORM-15341
|
Androgen Receptor
|
Endocrinology
|
|
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
|
-
- HY-100372
-
|
E4CPG
(RS)-ECPG
|
mGluR
|
Neurological Disease
|
|
E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation.
|
-
- HY-N2072
-
|
Transcrocetin
trans-Crocetin
|
iGluR
Endogenous Metabolite
|
Cancer
|
|
Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity. Transcrocetin (trans-Crocetin) is capable of crossing the blood-brain barrier and reach the central nervous system (CNS).
|
-
- HY-14854
-
|
Tecarfarin
ATI-5923
|
Others
|
Cardiovascular Disease
|
|
Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
|
-
- HY-111066A
-
|
JNJ-37822681 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
|
-
- HY-B0640A
-
-
- HY-B0480
-
-
- HY-13831
-
|
BPTU
BMS-646786
|
P2Y Receptor
|
Cancer
Neurological Disease
|
|
BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.
|
-
