Target Validation Information
TTD ID	T61722
Target Name	Prostaglandin D2 receptor 2 (PTGDR2)
Type of Target	Clinical trial
Drug Potency against Target	AZD1981	Drug Info	IC50 = 1.4~4 nM	[8]
	2-(2,4-diphenylthiazol-5-yl)acetic acid	Drug Info	IC50 = 870 nM	[7]
	2-(2-acetyl-4-bromophenoxy)acetic acid	Drug Info	IC50 = 4520 nM	[2]
	2-(2-allyl-4-chlorophenoxy)acetic acid	Drug Info	Ki = 5130 nM	[4]
	2-(2-benzhydryl-4-phenylthiazol-5-yl)acetic acid	Drug Info	IC50 = 370 nM	[6]
	2-(2-benzoyl-4-bromophenoxy)acetic acid	Drug Info	IC50 = 437 nM	[2]
	2-(2-cyclohexyl-4-fluorophenoxy)acetic acid	Drug Info	Ki = 446 nM	[4]
	2-(2-cyclohexyl-4-methoxyphenoxy)acetic acid	Drug Info	Ki = 782 nM	[4]
	2-(2-cyclohexyl-4-methylphenoxy)acetic acid	Drug Info	Ki = 353 nM	[4]
	2-(2-cyclohexylphenoxy)acetic acid	Drug Info	Ki = 311 nM	[4]
	2-(2-formylphenoxy)acetic acid	Drug Info	IC50 = 1970 nM	[2]
	2-(4-bromo-2-(hydroxymethyl)phenoxy)acetic acid	Drug Info	IC50 = 6870 nM	[2]
	2-(4-bromo-2-cyclohexylphenoxy)acetic acid	Drug Info	Ki = 83 nM	[4]
	2-(4-bromo-2-formylphenoxy)acetic acid	Drug Info	IC50 = 481 nM	[2]
	2-(4-bromo-2-tert-butylphenoxy)acetic acid	Drug Info	IC50 = 423 nM	[2]
	2-(4-chloro-2-cycloheptylphenoxy)acetic acid	Drug Info	IC50 = 248 nM	[5]
	2-(4-chloro-2-cyclohexylphenoxy)acetic acid	Drug Info	Ki = 154 nM	[4]
	2-(4-chloro-2-cyclopentylphenoxy)acetic acid	Drug Info	Ki = 150 nM	[4]
	2-(4-cyano-2-cyclohexylphenoxy)acetic acid	Drug Info	Ki = 230 nM	[4]
	3-(4-chloro-2-cyclohexylphenoxy)propanoic acid	Drug Info	Ki = 799 nM	[4]
	4-(4-chloro-2-cyclohexylphenoxy)butanoic acid	Drug Info	Ki = 1990 nM	[4]
	L-888607	Drug Info	Ki = 0.8 nM	[1]
	LAROPIPRANT	Drug Info	Ki = 745 nM	[3]
	Methyl 2-(4-chloro-2-cyclohexylphenoxy)acetate	Drug Info	Ki = 3280 nM	[4]
References
REF 1	Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. J Med Chem. 2005 Oct 6;48(20):6174-7.
REF 2	Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J Med Chem. 2006 Nov 16;49(23):6638-41.
REF 3	Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.
REF 4	2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50.
REF 5	7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8.
REF 6	Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5.
REF 7	Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80.
REF 8	Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1638-41.

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