Picotamide is a combined inhibitor of thromboxane A2 (TxA2) synthase and receptor. Picotamide has antiplatelet activity. Picotamide promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques in diabetes. Picotamide can be used for researching acute or chronic cardiovascular diseases.

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

Nivasorexant is a potent orexin receptor antagonist.

TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.

BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM.

Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia (extracted from patent US20150290125A1/US20110091459A1).

Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.

Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.

Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.

A small molecule compound of prostaglandin D2（PGD2) inhibitor.

ASP8302 (ASP 8302) is a potent, selective, positive allosteric modulator (PAM) of muscarinic M3 receptor.Threonine 230 (Thr 230) is the amino acid essential for the PAM effect of ASP8302.

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

Flupenthixol dihydrochloride is a typical antipsychotic of the thioxanthene class that acts as an antagonist at dopamine D2 receptors (Ki = 0.38 nM) and an inverse agonist at serotonin 5-HT2A receptors (Ki = 7 nM).1 It has also been identified as an inhib

Icalcaprant is a kappa-opioid receptor antagonist.

Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.

Protokylol hydrochloride(Caytine hydrochloride, JB-251 hydrochloride) is a salt form of protokylol and is an agonist of β-adrenergic receptor. Protokylol hydrochloride is also used as a bronchodilator.

RGH-122 is a potent, selective, and orally bioavailable V1a receptor antagonist with Ki/IC50 of 0.3/0.9 nM (hV1a) respectively, >100-fold selectiive over V2 receptor.

OPC-61815 is a water-soluble phosphate ester pro-drug of Tolvaptan (Cat# PC-45125), which is an orally active vasopressin V2 receptor antagonist.

SYD5115 (SYD-5115) is a potent, selective and orally bioavailable thyrotropin receptor (TSH-R) antagonist with IC50 of 48 and 62 nM for rTSHR and hTSHR, respectively.

CRN02481 is a potent and selective SST5 receptor agonist with EC50 of 0.37 nM (human SST5), with excellent selectivity against SST1, SST2, SST3 and SST4 receptors.

RC-752 is a potent, seletive sigma-1 receptor (S1R) antagonist with Ki of 6.2 nM, 50-fold selective over S2R, shows antinociceptive activity.

MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM.

GM310 is a small molecule inhibitor of glycolysis, proteotoxicity, inflammation, and impairments in animal models of Alzheime's, Huntington's, and stroke by activation of the Sigma-1 receptor.

CM-304 is a potent, selective sigma-1 receptor (S1R) antagonist with Ki of 3.41 nM, 100-fold selective over S2R.

AZ-66 is a highly potent S1R/S2R antagonist with Ki of 0.31/1.76 nM, respectively.

DC591053 (DC 591053) is a selective small molecule agonist of relaxin family peptide receptor 4 (RXFP4) with pEC50  of 7.24  and pKi  of  6.95, shows no activity against RXFP3.