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.

Ogremorphin-1 (OGM1) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.16 uM.

TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM.

NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.

1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM.

TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.

ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50.