| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T15571 | ||||
| Target Name | 5-HT 5A receptor (HTR5A) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | (+/-)-nantenine | Drug Info | Ki = 2224 nM | [5] | |
| (R)-zacopride | Drug Info | Ki = 16000 nM | [1] | ||
| 3,4-dihydroquinazolin-2-amine hydrobromide | Drug Info | Ki = 658 nM | [2] | ||
| 4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 24 nM | [2] | ||
| 4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 153 nM | [3] | ||
| 4-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 805 nM | [2] | ||
| 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 43 nM | [2] | ||
| 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 99 nM | [2] | ||
| 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 84.4 nM | [2] | ||
| 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 5.1 nM | [2] | ||
| 8-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 892 nM | [2] | ||
| 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 6.3 nM | [2] | ||
| METHIOTHEPIN | Drug Info | Ki = 1 nM | [1] | ||
| N,4-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 103 nM | [3] | ||
| N,N-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 2800 nM | [2] | ||
| N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 189 nM | [3] | ||
| SEROTONIN | Drug Info | IC50 = 184 nM | [4] | ||
| References | |||||
| REF 1 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812. | ||||
| REF 2 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. | ||||
| REF 3 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6. | ||||
| REF 4 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69. | ||||
| REF 5 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | ||||
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