Target Validation Information
TTD ID	T00884
Target Name	C-X-C chemokine receptor type 1 (CXCR1)
Type of Target	Successful
Drug Potency against Target	Reparixin	Drug Info	Ki = 1 nM	[3]
	SCH-527123	Drug Info	Ki = 3.9 nM	[5]
	(R)-2-(4-Isobutyl-phenyl)-N-methoxy-propionamide	Drug Info	IC50 = 1.8 nM	[4]
	1-(2-Bromo-phenyl)-3-(2,4-dihydroxy-phenyl)-urea	Drug Info	IC50 = 22 nM	[2]
	1-(2-hydroxy-4-nitrophenyl)-3-phenylurea	Drug Info	IC50 = 18200 nM	[1]
	Ibuprofen	Drug Info	IC50 = 110 nM	[4]
	R-ketoprofen	Drug Info	IC50 = 34 nM	[4]
	Reparixin	Drug Info	IC50 = 5.3 nM	[4]
Action against Disease Model	SCH-527123	Drug Info	Scientists at the National Institutes of Health (NIH) have developed h uMan embryonic kidney (HEK) 293 cell lines that express the CXCR1 chemokine receptor
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	Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleuki... Bioorg Med Chem Lett. 2004 Aug 16;14(16):4307-11.
REF 3	Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.
REF 4	2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors. J Med Chem. 2005 Jun 30;48(13):4312-31.
REF 5	Chemokine receptor antagonists: overcoming developmental hurdles. Nat Rev Drug Discov. 2009 Jan;8(1):23-33.

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