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

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.

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

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

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.

JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.

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.

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.

WLB-89462 (WLB89462) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 13 nM, >100-fold selective over σ1R (Ki=1777 nM).

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.

S6821 (S 6821) is a potent and selective bitter taste receptor TAS2R8 with IC50 of 21 nM.

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

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.

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

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.

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.

DF3016A (DF 3016A) is a potent and selective C5aR inhibitor with IC50 of 50 nM (C5a-induced human PMN migration and IC50 of 45 and 37 nM against rat and mouse C5aR, respectively.

T-ALZ01 (CMP-1696) is a small molecule inhibitor of complement component C1r.

Peptide WWGKKYRASKLGLAR is a super agonist of complement factor C3aR, 12-15 times more active than natural C3a.

MK-886 (L-663,536) is a potent, selective and orally active inhibitor of 5-lipoxygenase-activating protein (FLAP) with IC50 of 30 nM.

Rytvela (Peptide 101.10) is a potent, selective, allosteric negative modulator (antagonist) of IL-1 receptor I (IL-1RI), inhibits dose-dependently IL-1-induced PGE2 formation (IC50= 0.5 nM) and IL-1-induced human thymocyte (TF-1 cell) proliferation (IC50=

KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.