| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T46828 | ||||
| Target Name | D(1B) dopamine receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | 1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine | Drug Info | Ki = 43 nM | [1] | |
| 1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine | Drug Info | Ki = 951 nM | [1] | ||
| FLUMEZAPINE | Drug Info | IC50 = 20 nM | [2] | ||
| 1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one | Drug Info | Ki = 330 nM | [3] | ||
| (+/-)-nantenine | Drug Info | Ki = 2397 nM | [4] | ||
| FLUTROLINE | Drug Info | IC50 = 14 nM | [5] | ||
| 4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine | Drug Info | Ki = 366 nM | [1] | ||
| ISOLOXAPINE | Drug Info | IC50 = 2480 nM | [6] | ||
| ISOCLOZAPINE | Drug Info | IC50 = 758 nM | [7] | ||
| STEPHOLIDINE | Drug Info | Ki = 4.4 nM | [8] | ||
| Phenyltoloxamine | Drug Info | Ki = 414 nM | [1] | ||
| 1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine | Drug Info | IC50 = 1500 nM | [7] | ||
| 1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine | Drug Info | Ki = 113 nM | [1] | ||
| References | |||||
| REF 1 | J Med Chem. 2004 Aug 12;47(17):4155-8.Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity. | ||||
| REF 2 | J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. | ||||
| REF 3 | Bioorg Med Chem. 2007 Sep 1;15(17):5811-8. Epub 2007 Jun 7.Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand. | ||||
| REF 4 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
| REF 5 | J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. | ||||
| REF 6 | J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. | ||||
| REF 7 | J Med Chem. 1982 Jul;25(7):855-8.Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. | ||||
| REF 8 | Bioorg Med Chem. 2009 Oct 1;17(19):6898-907. Epub 2009 Aug 20.Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?. | ||||
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