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.

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

MP135 is a potent, μ-δ opioid receptor heteromer-selective agonist with EC50 of 0.8 nM in GTPγS assays, shows functional selectivity for μ-δ heteromers over homomeric μOR and δOR and low β-arrestin2 recruitment activity.

LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding.

AT-039 is a potent, selective agonist of nociceptin opioid peptide (NOP) receptor, AT-039 is useful for treatment of hypertension and/or volume overload/hyponatraemic states.

ML301 is a selective full (79-93%) neurotensin-1 (NTR1) receptor agonist with EC50 of 2.0-4.1 uM, good selectivity relative to NTR2 and GPR35.

VU0506013 is a high-affinity, selective positive allosteric modulator (PAM) of neuropeptide Y4 receptor (Y4R) with EC50 of 125 nM.

VU6046980 is a potent, selective and in vivo active mGlu7 positive allosteric modulator (PAM) with EC50 of 0.15 uM (rat mGlu7).

MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8.

CVN636 is a potent, selective, CNS penetrant and allosteric agonist of mGluR7 with EC50 of 7 and 2 nM for human and mouse mGluR7, respectively.

TCMCB07 is a synthetic, cyclic nonapeptide peptide antagonist of the melanocortin-4 receptor (MC4R), ameliorates cancer- and chronic kidney disease-associated cachexia.

SNT-207858 (SNT207858) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 22/11 nM, respectively.