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].

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].

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.

YE 120 is a highly potent GPR35 agonist (EC50: 32.5 nM) with potential anti-inflammatory and anti-cancer activities, which can be used to study G protein-coupled receptor-related diseases.

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.

Pamoic acid disodium is a GPR35 agonist.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.

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

TM-N1324 is a GPR39 agonist. TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies to murine GPR39 with EC50s of 180 nM and 5 nM, respectively.

Tyrphostin A25 (Tyrphostin AG 82) is a specific EGFR tyrosine kinase inhibitor and GPR35 agonist with an IC50 value of 0.94 μM for GPR35 and an EC50 value of 5.3 μM for GPR35.

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].

TC-G-1008 (GPR39-C3) is a zinc receptor agonist with EC50 values of 0.4 nM for rat GPR39 and 0.8 nM for human GPR39.

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35/CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

NSC-299202 is a novel potent agonist of Human G Protein-Coupled Receptor-35 (hGPR35) (EC50 8 nM).

YL-365 is a highly potent and selective GPR34 antagonist that exhibits excellent activity in neuropathic pain models for the study of neurologic diseases.