GSK2239633A

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96.

Product Specifications

CAS Number

[1240516-71-5]

UNSPSC

12352005

Target

CCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/GSK2239633A.html

Purity

99.81

Solubility

DMSO : ≥ 250 mg/mL

Smiles

CC(C)(O)C(NCC1=CC=CC(CN2N=C(NS(=O)(C3=CC=C(Cl)S3)=O)C4=C2C=CC=C4OC)=C1)=O

Molecular Formula

C24H25ClN4O5S2

Molecular Weight

549.06

References & Citations

[1]Cahn A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol. 2013 Feb 28;14:14.|[2]Slack RJ, et al. Antagonism of human CC-chemokine receptor 4 can be achieved through three distinct binding sites on the receptor. Pharmacol Res Perspect. 2013 Dec;1 (2) :e00019.|[3]Miah AH, et al. Identification of pyrazolopyrimidine arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists. Bioorg Med Chem. 2017 Oct 15;25 (20) :5327-5340.