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.

SNT-207707 (SNT207707) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 8/5 nM, respectively.

VU0405645 is a potent, biased M1 receptor-positive allosteric modulator, potentiates Ca2+ mobilization in CHO cells stably expressing the M1 receptor with EC50 of 340 nM.

UCM-14216 (UCM14216) is a potent and selective antagonist of type 2 lysophosphatidic acid receptor (LPA2) with KD value of 1.3 nM and IC50 of 1.9 uM.

TP0541640 (TP 0541640) is a novel potent LPA1 antagonist with IC50 of 1.6 nM, shows potential for the treatment of lung and skin fibrosis.

SLB1122168 hydrochloride is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

SLB1122168 is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

NXC736 hydrochloride (SLB736) is a selective functional antagonist for type 4 sphingosine-1-phosphate receptor (S1PR4), has immunomodulatory and anti-fibrotic effects.

IMMH002 is a potent, selective and orally active S1P1 agonist, IMMH002 can be transformed to IMMH002-P in vivo, IMMH002-P activates S1P1, S1P4, and S1P5 with 12.4, 19.8 and 29.4 nM respectively.

ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.

LY290154 is a leukotriene LTD4/E4 antagonist.

UR-MB-69 is a potent agonist of histamine H2 receptor (H2R) dopamine receptor D3R with pKi of 8.69 and 8.06, respectively.

RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.

RTI-122 (RTI 122) is a highly potent, selective and brain permeable GPR88 agonist with cAMP EC50 of 11 nM (hGPR88 CHO).

OX04529 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 18.5 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.

OX04528 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 5.98 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.