gpr3

GPR3 agonist-2 (compound 32) is a potent full agonist of the G protein-coupled receptor 3 (GPR3), exhibiting an IC50 value of 260 nM [1].

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

GPR35 agonist 1 is a highly effective and specific GPR35 CXCR8 agonist (EC50: 5.8 nM).

Gpr35modulator 3 (Example 105) is a Gpr35 regulator with an IC50 of less than 1 μM. It is utilized in research related to proliferation, immune response, and inflammation.

Gpr35modulator 2 (compound 52) serves as a modulator for GPR35. It is utilized in researching a variety of diseases related to GPR35.

Gpr35modulator 1 (compound 1-18) acts as an effective modulator of Gpr35, demonstrating an IC50 of less than or equal to 100 nM in HEK293 cells stably transfected with human GPR35.

GPR35activator-1 (example 5) is an effective activator of GPR35, exhibiting a Ki of 0.08 nM for human GPR35.

GPR30 agonist-1 is a compound that acts as an agonist for G protein-coupled receptor 30 (GPR30), inducing vasorelaxation.

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1 2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

Compound 6 (3,5-dinitro-bisphenol A), also known as GPR35 agonist 5, exhibits weak GPR35 agonistic activity. This compound causes G1 Go phase arrest in CHO-S cells [1].

Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As an intracellular second messenger, it mobilizes Ca2+ and acts as an extracellular ligand for G-protein coupled receptors. This important lipid mediator is generated from sphingosine or other membrane phospholipids.

Oleic acid (Glycon Wo) is a natural product, a common monounsaturated fatty acid found in a variety of animal and vegetable fats and oils. Palmitic acid is a Na+ K+ ATPase activator.

O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment of cystitis.O-1602 promotes hepatic steatosis through GPR55 and PI3 kinase Akt SREBP-1c signalling in mice.O-1602 induces, in a GPR3-independent manner, in Hep55B cells with elevated intracellular calcium.

UR-MB-355, a GPR3 ligand, demonstrates submicromolar affinities for its primary target GPR3 and the closely related receptors GPR6 and GPR12 [1].

AF64394 is a selective inverse agonist of GPR3(pIC50 : 7.3)