CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM.

CCX-6239 is a novel potent, orally available CCR4 inhibitor with potential utility in the treatment of allergic airways disease.

CJ-1639 (CJ1639) is a potent, highly selective dopamine D3 receptor (D3R) full agonist with Ki of 0.5 nM, >5,000-fold selectivity over D1 and D2 receptors in binding assays.CJ-1639 binds to human D3 receptor with a K(i) value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 receptors.CJ-1639 is an excellent pharmacological tool to elucidate the role of the D3 receptor in different neurological conditions in animal models.

Cotadutide (MEDI-0382) is a dual GLP-1/glucagon receptor peptide agonist with robust anti-obesity and metabolic effects.

CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.

CXCR7 modulator 20 is a small molecule modulator of the atypical chemokine receptor CXCR7 with Ki of 52 nM.

DA-1241 (DA1241) is a novel potent, highly selective GPR119 agonist, activates human GPR119 (EC50=4.37 nM) in increasing cAMP levels in GPR119-overexpressing HEK293 cells.DA-1241 increased cAMP levels via activated mouse GPR119 (EC50, 71.5 nM) and rat GPR119 (EC50, 156 nM).DA-1241 showed no significant activity against 156 off-target proteins at 10 uM, including human GLP-1 receptor and human GPR40.DA-1241 stimulated insulin secretion in hamster insulinoma HIT-T15 cells with EC50 of 22.3 nM, association with enhanced human insulin promoter activity.DA-1241 significantly reduced postprandial glucose excursion, significantly preserved β-cell mass with reduced PDX1 levels in the islets from HFD/STZ diabetic mice.DA-1241 reduced triglyceride content in the liver thereby improved fatty liver, reduced gluconeogenic enzyme expression in HepG2 cells and mouse liver, reduced autophagic flow in HepG2 cells.

DCP1-3 is a novel allosteric ligand of the angiotensin receptor AT1R, displays NAM potency on AngIV with IC50 of 0.29 uM.DCP1-3 reduces AngII-induced contraction in renal and iliac arteries in mice.DCP1-3 inhibits IgG binding to HEK-AT1R cells with IC50 of 2.9 nM.DCP1-3 reverses PAM effect of the IgG on the agonist-induced calcium response.

DL-175 is a potent and selective biased GPR84 agonist with EC50 of 33 nM.DL-175 exhibits no significant activity in a panel of 168 other GPCRs.DL-175 display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells.DL-175 markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement.

DPC168 (DPC-168) is a highly potent, selective CC chemokine receptor-3 (CCR3) antagonist with IC50 of 2.0 nM, inhibits eotaxin-induced chemotaxis with IC50 of 0.034 nM.DPC168 demonstrates potency for mouse CCR3 (chemotaxis IC50=41 nM) and oral bioavailability in mice (20% F).DPC168 reduced eosinophil recruitment into the lungs in a dose-dependent manner in these animal models.

EMU-116 (EMU-000116) is a potent, selective CXCR4 antagonist with IC50 29.6 nM in Ca2+ flux assay.

Enerisant (S091,TS-091) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

Enerisant hydrochloride (TS091 hydrochloride) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling; blocks TNFα production in synovial explants from patients with arthritis, and inhibits mast cell tryptase-induced recruitment of eosinophils into the pleural cavity of mice, dose dependently attenuates joint inflammation.

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.FE 205030 displays>100,000 fold against hAM1R and >6363 fold against hAM2R tested in Human CGRP, AM1R and AM2R receptor cAMP assays.FE 205030 inhibited CGRP-induced vasodilation in isolated human mesenteric resistance arteries in an ex vivo isometric myograph study; effectively blocked CGRP-induced vasodilation with a pA2 of 9.3.FE 205030 is a first in class injectable fast acting selective and potent agent for the treatment of acute episodic migraine.

FFA2R agonist 58 is a potent, allosteric FFAR2 (GPR43) agonist/modulator.FFA2R agonist 58 functions as a positive/priming modulator in these cells by turning the natural FFA2R agonist acetate into a potent activator of the neutrophil NADPH-oxidase.FFA2R agonist 58 lowers the concentration of acetate required to induce a transient rise in the concentration of intracellular Ca2+ in neutrophils, has no direct effect on the neutrophil NADPH-oxidase activity but affects the response induced by acetate.FFA2R agonist 58 significantly reduced the amount of internalized influenza A virus (IAV) in treated A549 cells.

Firazorexton is a potent, selective, experimental orexin 2 receptor (OX2R) agonist.

FLX-475 is a novel CCR4 antagonist for the treatment of cancer.

GnRH antagonist 2 is a GnRH receptor antagonist that can be used for endometriosis research.

GPR183 antagonist SAE-14 is a potent, selective GPR183 antagonist with IC50 of 28.5 nM, inhibits GPR183-dependent 7α,25-dihydroxycholesterol-induced calcium signaling in HL-60 cells.GPR183 antagonist SAE-14 inhibits calcium mobilization induced by 7α,25-OHC (EC80 209 nM).GPR183 antagonist SAE-14 reversed CCI-induced mechanical allodynia in a time-dependent manner when administered in vivo to mice.7α,25-dihydroxycholesterol induced allodynia in mice, SAE-14 blocked the effects of 7α,25-OHC in a dose-dependent manner.

GPR183 antagonist SAE-14 is a potent, selective GPR183 antagonist with IC50 of 8.3 nM, inhibits calcium mobilization induced by 7α,25-OHC in HL-60 cells.

GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor; displays >100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types; blocks porcine carotid vascular response to sumatriptan in vivo; orally bioavailable and centrally active.