Target Validation Information
Target ID T00884
Target Name High affinity interleukin-8 receptor A
Target Type
Clinical Trial
Drug Potency against Target 1-(2-Bromo-phenyl)-3-(2,4-dihydroxy-phenyl)-urea Drug Info IC50 = 22 nM [527139]
SCH-527123 Drug Info Ki = 3.9 nM [552901]
1-(2-hydroxy-4-nitrophenyl)-3-phenylurea Drug Info IC50 = 18200 nM [526980]
RAPARIXIN Drug Info IC50 = 5.3 nM [527602]
IBUPROPHEN Drug Info IC50 = 110 nM [527602]
(R)-2-(4-Isobutyl-phenyl)-N-methoxy-propionamide Drug Info IC50 = 1.8 nM [527602]
R-KETOPROFEN Drug Info IC50 = 34 nM [527602]
Reparixin Drug Info Ki = 1 nM [527153]
Action against Disease Model SCH-527123 Scientists at the National Institutes of Health (NIH) have developed h uMan embryonic kidney (HEK) 293 cell lines that express the CXCR1 chemokine receptor Drug Info
References
Ref 527139Bioorg Med Chem Lett. 2004 Aug 16;14(16):4307-11.Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8(IL-8) receptor antagonists.
Ref 552901Chemokine receptor antagonists: overcoming developmental hurdles. Nat Rev Drug Discov. 2009 Jan;8(1):23-33. doi: 10.1038/nrd2734. Epub 2008 Dec 12.
Ref 526980J Med Chem. 2004 Mar 11;47(6):1319-21.Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
Ref 527602J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Ref 527602J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Ref 527602J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Ref 527602J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Ref 527153Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6. Epub 2004 Jul 28.Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury.

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