| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T26500 | ||||
| Target Name | Histamine H4 receptor | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | A-846714 | Drug Info | Ki = 35 nM | [529717] | |
| A-943931 | Drug Info | Ki = 4.7 nM | [529717] | ||
| (R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate | Drug Info | Ki = 290 nM | [530465] | ||
| (1H-indol-2-yl)(piperazin-1-yl)methanone | Drug Info | Ki = 38 nM | [527934] | ||
| 6-(4-Methylpiperazin-1-yl)pyrimidine-2,4-diamine | Drug Info | Ki = 290 nM | [530400] | ||
| 6-(4-Methylpiperazin-1-yl)-9H-purin-2-amine | Drug Info | Ki = 15600 nM | [530400] | ||
| IODOPHENPROPIT | Drug Info | Ki = 7.8 nM | [529455] | ||
| 2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole | Drug Info | Ki = 1.1 nM | |||
| 6-(4-methylpiperazin-1-yl)-9Hpurine | Drug Info | Ki = 18400 nM | [530400] | ||
| 9-benzyl-6-(4-methylpiperazin-1-yl)-9H-purine | Drug Info | Ki = 14300 nM | [530400] | ||
| References | |||||
| Ref 529717 | J 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. | ||||
| Ref 529717 | J 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. | ||||
| Ref 530465 | Bioorg 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. | ||||
| Ref 527934 | J 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. | ||||
| Ref 530400 | Bioorg 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. | ||||
| Ref 530400 | Bioorg 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. | ||||
| Ref 529455 | J 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. | ||||
| Ref 530400 | Bioorg 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. | ||||
| Ref 530400 | Bioorg 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. | ||||
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