Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR01193
Target NameHistamine H4 receptor    
Type of TargetResearch target    
Drug Potency against Target4-(2-(4-tert-butylphenylthio)ethyl)-1H-imidazoleKi = 1.1 nM[1]
JNJ-7777120Ki = 14 nM[2]
9-benzyl-6-(4-methylpiperazin-1-yl)-9H-purineKi = 14300 nM[2]
6-(4-Methylpiperazin-1-yl)-9H-purin-2-amineKi = 15600 nM[2]
(R)-(-)-alpha-methylhistamineKi = 184 nM[3]
6-(4-methylpiperazin-1-yl)-9HpurineKi = 18400 nM[2]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamateKi = 290 nM[4]
6-(4-Methylpiperazin-1-yl)pyrimidine-2,4-diamineKi = 290 nM[2]
A-846714Ki = 35 nM[5]
(1H-indol-2-yl)(piperazin-1-yl)methanoneKi = 38 nM[6]
JNJ-7777120Ki = 38 nM[7]
A-943931Ki = 4.7 nM[5]
IODOPHENPROPITKi = 7.8 nM[3]
Ref 1Bioorg. Med. Chem. 18(14):5441-5448 (2010) To Reference
Ref 2Bioorg Med Chem. 2009 Oct 15;17(20):7186-96. Epub 2009 Sep 2.2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. To Reference
Ref 3J Med Chem. 2008 Jun 12;51(11):3145-53. Epub 2008 May 7.Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. To Reference
Ref 4Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5. Epub 2009 Oct 6.Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. To Reference
Ref 5J Med Chem. 2008 Oct 23;51(20):6547-57. Epub 2008 Sep 26.Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. To Reference
Ref 6J Med Chem. 2005 Dec 29;48(26):8289-98.Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. To Reference
Ref 7Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9. Epub 2010 Mar 3.Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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