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. | ||||
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