CMP-1611 is a small molecule inhibitor of protease of the complement classical pathway, C1r, directly inhibits classical pathway-specific complement activation in a dose-dependent manner.

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.

LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.

L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion.

CR6086 sodium (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.

AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors.

AGN 225660 is a second-generation prostanoid receptor antagonist acting at multiple receptor subtypes with IC50 of 220/70/2900/7100/70/180/1100/5 nM for DP1/EP1/EP2/EP3/EP4/FP/IP/TP receptors, respectively.

ACT-774312 (ACT774312) is a potent and selective CRTH2 receptor antagonist with IC50 of 3 nM, 150-fold more potent than setipiprant in inhibiting PGD2-induced eosinophil cell shape change.

MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM).

MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R).

OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A.

CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).

ZYKR1 is a potent, and peripherally restricted kappa opioid receptor (KOR)-selective agonist with EC50 of 0.061 nM in cAMP assays, highly selective over the mu and delta opioid receptors (EC50>10 μM).

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.

PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response.