Target Validation Information
TTD ID	T56923
Target Name	C-X-C chemokine receptor type 2 (CXCR2)
Type of Target	Successful
Drug Potency against Target	Reparixin	Drug Info	IC50 = 1 nM	[7]
	SB-656933	Drug Info	IC50 = 5.1 nM	[6]
	SCH-527123	Drug Info	Ki = 2.6 nM	[5]
	(R)-2-(4-Isobutyl-phenyl)-N-methoxy-propionamide	Drug Info	IC50 = 1.8 nM	[2]
	1-(2-bromophenyl)-3-(4-cyano-2-hydroxyphenyl)urea	Drug Info	IC50 = 25 nM	[4]
	1-(2-Hydroxy-3-nitro-phenyl)-3-phenyl-urea	Drug Info	IC50 = 860 nM	[1]
	1-(2-hydroxy-4-nitrophenyl)-3-phenylurea	Drug Info	IC50 = 320 nM	[4]
	1-(2-Hydroxy-5-nitro-phenyl)-3-phenyl-urea	Drug Info	IC50 = 10900 nM	[1]
	1-(3-cyano-2-hydroxyphenyl)-3-phenylurea	Drug Info	IC50 = 276 nM	[4]
	1-(4-cyano-2-hydroxyphenyl)-3-phenylurea	Drug Info	IC50 = 200 nM	[4]
	1-(5-chloro-2-hydroxy-4-nitrophenyl)-3-phenylurea	Drug Info	IC50 = 950 nM	[4]
	5-(pentylthio)thiazolo[4,5-d]pyrimidin-7-ol	Drug Info	IC50 = 10000 nM	[3]
	Ibuprofen	Drug Info	IC50 = 110 nM	[2]
	R-ketoprofen	Drug Info	IC50 = 34 nM	[2]
	Reparixin	Drug Info	IC50 = 5.3 nM	[2]
Action against Disease Model	SCH-527123	Drug Info	In a h uMan neutrophil (hPMN) chemotaxis assay, SCH 527123 displayed superior inhibition of chemotaxis in vitro induced by CXCL1 or CXCL8. SCH 527123 demonstrated complete inhibition of CXCL1-mediated neutrophil chemotaxis at 2 nM, while inhibition of CXCL8-mediated chemotaxis was less potent	[5]
References
REF 1	Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor. J Med Chem. 2004 Mar 11;47(6):1319-21.
REF 2	2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors. J Med Chem. 2005 Jun 30;48(13):4312-31.
REF 3	Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):960-3.
REF 4	Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1713-7.
REF 5	Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist. J Med Chem. 2006 Dec 28;49(26):7603-6.
REF 6	CXCR2 antagonists for the treatment of pulmonary disease. Pharmacol Ther. 2009 Jan;121(1):55-68.
REF 7	Chemokine receptor antagonists: overcoming developmental hurdles. Nat Rev Drug Discov. 2009 Jan;8(1):23-33.

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