Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T62184 | ||||
Target Name | GABA transporter GAT-1 (SLC6A1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | (R)-nipecotic acid | Drug Info | IC50 = 2600 nM | [1] | |
(S)-Piperidine-3-carboxylic acid | Drug Info | IC50 = 2660 nM | [1] | ||
2,4-Diamino-butyric acid(GABA) | Drug Info | IC50 = 2000 nM | [2] | ||
4-Hydroxy-piperidine-3-carboxylic acid | Drug Info | IC50 = 11000 nM | [3] | ||
GSK683699 | Drug Info | IC50 = 2640 nM | [1] | ||
References | |||||
REF 1 | Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling. J Med Chem. 2004 Nov 4;47(23):5620-9. | ||||
REF 2 | Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions. J Med Chem. 1986 Feb;29(2):224-9. | ||||
REF 3 | Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors. J Med Chem. 1982 Oct;25(10):1157-62. | ||||
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