Target Validation Information
Target ID T61722
Target Name Putative G-protein coupled receptor 44
Target Type
Clinical Trial
Drug Potency against Target 2-(2-formylphenoxy)acetic acid Drug Info IC50 = 1970 nM [528566]
2-(4-bromo-2-formylphenoxy)acetic acid Drug Info IC50 = 481 nM [528566]
2-(2-cyclohexyl-4-methoxyphenoxy)acetic acid Drug Info Ki = 782 nM [528862]
2-(2-benzoyl-4-bromophenoxy)acetic acid Drug Info IC50 = 437 nM [528566]
3-(4-chloro-2-cyclohexylphenoxy)propanoic acid Drug Info Ki = 799 nM [528862]
2-(4-cyano-2-cyclohexylphenoxy)acetic acid Drug Info Ki = 230 nM [528862]
2-(4-bromo-2-cyclohexylphenoxy)acetic acid Drug Info Ki = 83 nM [528862]
2-(2-cyclohexylphenoxy)acetic acid Drug Info Ki = 311 nM [528862]
2-(4-chloro-2-cyclohexylphenoxy)acetic acid Drug Info Ki = 154 nM [528862]
2-(2-cyclohexyl-4-methylphenoxy)acetic acid Drug Info Ki = 353 nM [528862]
4-(4-chloro-2-cyclohexylphenoxy)butanoic acid Drug Info Ki = 1990 nM [528862]
2-(2-cyclohexyl-4-fluorophenoxy)acetic acid Drug Info Ki = 446 nM [528862]
2-(4-bromo-2-tert-butylphenoxy)acetic acid Drug Info IC50 = 423 nM [528566]
AZD1981 Drug Info IC50 = 1.4~4 nM [553017]
2-(4-chloro-2-cycloheptylphenoxy)acetic acid Drug Info IC50 = 248 nM [530255]
L-888607 Drug Info Ki = 0.8 nM [527768]
LAROPIPRANT Drug Info Ki = 745 nM [528672]
2-(4-bromo-2-(hydroxymethyl)phenoxy)acetic acid Drug Info IC50 = 6870 nM [528566]
2-(2-benzhydryl-4-phenylthiazol-5-yl)acetic acid Drug Info IC50 = 370 nM [530588]
2-(2,4-diphenylthiazol-5-yl)acetic acid Drug Info IC50 = 870 nM [530594]
2-(2-acetyl-4-bromophenoxy)acetic acid Drug Info IC50 = 4520 nM [528566]
Methyl 2-(4-chloro-2-cyclohexylphenoxy)acetate Drug Info Ki = 3280 nM [528862]
2-(2-allyl-4-chlorophenoxy)acetic acid Drug Info Ki = 5130 nM [528862]
2-(4-chloro-2-cyclopentylphenoxy)acetic acid Drug Info Ki = 150 nM [528862]
The Effect of Target Knockout, Knockdown or Genetic Variations CRTH2(-/-) mice and wild-type control animals were epicutaneously sensitized by means of repeated application of ovalb uMin (OVA) to tape-stripped skin for 7 weeks and then challenged by means of OVA application to tape-stripped previously unsensitized skin for 1 week. Skin histology was assessed by means of hematoxylin and eosin staining and immunohistochemistry. Cytokine mRNA expression was examined by means of quantitative RT-PCR. Levels of PGD?, antibody, and cytokines were measured by means of ELISA.PGD2 levels significantly increased in skin 24 hours after tape stripping, although not in skin subjected to repeated sensitization with OVA. Allergic skin inflammation developed normally at sites of chronic epicutaneous sensitization with OVA in CRTH2(-/-) mice but was severely impaired in previously unsensitized skin challenged with OVA, as evidenced by significantly decreased skin infiltration with eosinophils and CD4(+) cells and impaired T(H)2 cytokine mRNA expression. Impaired skin inflammation at sites of acute OVA challenge in CRTH2(-/-) mice was not due to an impaired systemic response to epicutaneous sensitization because OVA-specific IgG1 and IgE antibody levels and OVA-driven splenocyte secretion of cytokines in these mice were comparable with those seen in wild-type control animals.CRTH2 promotes allergic skin inflammation in response to cutaneous exposure to antigen in previously sensitized mice [528566]
References
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 553017Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1638-41. doi: 10.1016/j.bmcl.2010.01.092. Epub 2010 Jan 22.
Ref 530255Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. Epub 2009 Jun 14.7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Ref 527768J Med Chem. 2005 Oct 6;48(20):6174-7.Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Ref 528672J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 530588Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5. Epub 2009 Dec 6.Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
Ref 530594Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80. Epub 2009 Dec 4.Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
Ref 528566J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Ref 528862Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.

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