GPCR

GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.

Fulvestrant-d3 is a isotope labeled compound of Fulvestrant.Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist and GPR30 agonist that inhibits cell proliferation and induces apoptosis and autophagy.

CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease.

TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.

NOX-6-18 (GPR132-B-160) is a highly potent and selective GPR132 antagonist with insulinotropic activity that modulates macrophage reprogramming in pancreatic islets and reduces weight gain.

TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a phenylpyridone derivative with MCH1R Ki of 3.4 nM against human. In mice, MCH1R Ki was 3.0 nM.

CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.

BTB09089 (GPR65 agonist ) is a T cell death-associated gene 8 (TDAG8/GPR65)-specific agonist.BTB09089 induces TDAG8 expression and regulates cytokine production in T cells and macrophages.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

ONC212 [a fluorinated-ONC201 analogue] is a selective GPR132 agonist.

AZD1979 is a highly potent MCHR1 (Melanin-concentrating hormone receptor 1) antagonist with an IC50 of 12 nM, exhibiting improved central nervous system (CNS) exposure and enhanced insulin sensitivity in steady-state model assessments, making it suitable for the treatment of obesity.

Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.

LY2881835 is a potent and selective GPR40 agonist.

AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

Tetrahydromagnolol can activate cannabinoid (CB) receptors.

BIM-46174 HCl is a selective G protein inhibitor with anticancer activity that inhibits the growth of a large number of human cancer cell lines and induces cysteine 3-dependent apoptosis.

HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68 with an EC50 of 170 nM, used in the study of autoimmune chronic inflammatory diseases [1].