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 [527160]
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine Drug Info Ki = 951 nM [527160]
FLUMEZAPINE Drug Info IC50 = 20 nM [533515]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one Drug Info Ki = 330 nM [528904]
(+/-)-nantenine Drug Info Ki = 2397 nM [530558]
FLUTROLINE Drug Info IC50 = 14 nM [533512]
4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine Drug Info Ki = 366 nM [527160]
ISOLOXAPINE Drug Info IC50 = 2480 nM [533577]
ISOCLOZAPINE Drug Info IC50 = 758 nM [533570]
STEPHOLIDINE Drug Info Ki = 4.4 nM [530374]
Phenyltoloxamine Drug Info Ki = 414 nM [527160]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine Drug Info IC50 = 1500 nM [533570]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine Drug Info Ki = 113 nM [527160]
References
Ref 527160J 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 527160J 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 533515J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
Ref 528904Bioorg 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 530558Bioorg 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 533512J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.
Ref 527160J 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 533577J 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 533570J 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 530374Bioorg 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?.
Ref 527160J 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 533570J 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 527160J 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.

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