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GPR88 receptor agonist
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay. -
CGRP antagonist
Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. -
Smo receptor agonist
SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM. -
triple reuptake inhibitor
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. -
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. -
CB1 receptor inverse agonist
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist. -
5-HT1F receptor agonist
LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist. -
5-HT1F agonist
LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM. -
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). -
D1/D5 receptor full agonist
SKF-82958 hydrobromide is a D1/D5 receptor full agonist. -
ghrelin receptor inverse agonist
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36. -
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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GPR40 agonist
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. - Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
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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. -
immune modulator
Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55). -
guanylate cyclase (GC) activator
Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets. -
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). -
Smo allosteric activator
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells. -
CXCR3 antagonist
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. -
SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. -
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. -
mGluR5 positive allosteric modulator
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation . -
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. -
DPP4 inhibitor
Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1). -
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. -
δ opioid receptor agonist
AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2??0.9 nM for δ agonist potency. -
5-HT1B receptor antagonist
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. -
dopamine reuptake inhibitor
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). -
non-peptide nociceptin receptor (NOP) agonist
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention. -
partial mGluR4 agonist
(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM. -
LTC4 inhibitor
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2). -
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). -
D1-like dopamine receptor (D1/D5) agonist
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. -
beta-adrenoceptor agonist
Bambuterol ((??)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.

