Target Validation Information
TTD ID T26500
Target Name Histamine H4 receptor (H4R)
Type of Target
Clinical trial
Drug Potency against Target (1H-indol-2-yl)(piperazin-1-yl)methanone Drug Info Ki = 38 nM [1]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info Ki = 290 nM [5]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Drug Info Ki = 1.1 nM
6-(4-Methylpiperazin-1-yl)-9H-purin-2-amine Drug Info Ki = 15600 nM [4]
6-(4-methylpiperazin-1-yl)-9Hpurine Drug Info Ki = 18400 nM [4]
6-(4-Methylpiperazin-1-yl)pyrimidine-2,4-diamine Drug Info Ki = 290 nM [4]
9-benzyl-6-(4-methylpiperazin-1-yl)-9H-purine Drug Info Ki = 14300 nM [4]
A-846714 Drug Info Ki = 35 nM [3]
A-943931 Drug Info Ki = 4.7 nM [3]
[125I]iodophenpropit Drug Info Ki = 7.8 nM [2]
References
REF 1 Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem. 2005 Dec 29;48(26):8289-98.
REF 2 Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. J Med Chem. 2008 Jun 12;51(11):3145-53.
REF 3 Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and... J Med Chem. 2008 Oct 23;51(20):6547-57.
REF 4 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. Bioorg Med Chem. 2009 Oct 15;17(20):7186-96.
REF 5 Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.