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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