Target Validation Information
Target ID T62184
Target Name Sodium- and chloride-dependent GABA transporter 1
Target Type
Successful
Drug Potency against Target 4-Hydroxy-piperidine-3-carboxylic acid Drug Info IC50 = 11000 nM [533544]
(S)-Piperidine-3-carboxylic acid Drug Info IC50 = 2660 nM [527271]
2,4-Diamino-butyric acid(GABA) Drug Info IC50 = 2000 nM [533404]
(R)-Piperidine-3-carboxylic acid Drug Info IC50 = 2600 nM [527271]
GAMMA-AMINO-BUTANOIC ACID Drug Info IC50 = 2640 nM [527271]
References
Ref 533544J Med Chem. 1982 Oct;25(10):1157-62.Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Ref 527271J Med Chem. 2004 Nov 4;47(23):5620-9.Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
Ref 533404J Med Chem. 1986 Feb;29(2):224-9.Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions.
Ref 527271J Med Chem. 2004 Nov 4;47(23):5620-9.Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
Ref 527271J Med Chem. 2004 Nov 4;47(23):5620-9.Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.

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