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MC1R and MC5R antagonist
JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells. -
α1A antagonist
RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8). -
NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
CGRP receptor antagonist
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
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CRF-1 antagonist
Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. -
5-HT6 receptor antagonist
SB 399885 is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
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DP1 receptor antagonist
Asapiprant, also known as S-555739, is a the potent and selective DP1 receptor antagonist. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. -
NK1 receptor antagonist
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. -
CXCR3 antagonist
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. -
angiotensin II receptor antagonist
Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist. -
Neurokinin-1 (NK-1) receptor antagonist
Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. -
angiotensin II type 1 receptor antagonist
Azilsartan D5 is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist. -
OT-R antagonist
OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 2 inhibitis IP3-Synthesis, rat OT-R (IC50 = 0.33 μM). -
adenosine A1 receptor antagonist
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. -
CGRP antagonist
Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. -
AT2R antagonist
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. -
CB1 antagonist/inverse agonist
Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1. -
SSTR5 antagonist
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM). -
LTB4 antagonist
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. -
μ-opioid receptor (MOR) antagonist
GSK1521498 hydrochloride is a potent and selective μ-opioid receptor (MOR) antagonist.
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mGlu5 receptor antagonist
Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist. -
β-adrenoceptor antagonist
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. -
LPA1 antagonist
BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. -
endothelin ETA and ETB receptor antagonist
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
CXCR3 antagonist
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. -
non-peptide CCR1 antagonist
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. -
5-HT7 receptor antagonist
SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors. -
mGlu5 receptor antagonist
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. -
CGRP1 receptor antagonist
Olcegepant hydrochloride is the first 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. -
5-HT1B receptor antagonist
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. -
EP4 antagonist
CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3). -
dopamine D2 receptor antagonist
Haloperidol D4 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist. -
5-HT2 receptor antagonist
Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. -
dopamine D2 receptor antagonist
Haloperidol-d4-1 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
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5-HT2 receptor antagonist
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. -
histamine H2-receptor antagonist
Niperotidine is a histamine H2-receptor antagonist. -
5-HT / dopamine receptor antagonist
Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
adenosine A1 receptor antagonist
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively.
GPCR/G Protein
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