[3H]GABA [Ligand Id: 5410] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL96 (4-aminobutyric acid, Aminobutyric acid, Aminobutyric acid, gamma-, Butyric acid, 4-amino-, Factor i, Gamma-aminobutyrate, .gamma.-amino-butyric acid, .gamma.-aminobutyric acid, Gamma-aminobutyric acid, .gamma.-amino-n-butyric acid, NSC-27418, Vigabatrin impurity, .gamma.-aminobutyric acid-)
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  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/GABA A receptor alpha-4/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2111366] [GtoPdb: 414, 412, 407] [UniProtKB: P18507, P28472, P48169]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
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  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
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  • GABAA receptor β3 subunit/GABAA receptor α3 subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 in Human [ChEMBL: CHEMBL3885574] [GtoPdb: 412, 406] [UniProtKB: P28472, P34903]
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  • GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABAA receptor θ subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta in Human [ChEMBL: CHEMBL3885575] [GtoPdb: 412, 406, 418] [UniProtKB: P28472, P34903, Q9UN88]
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  • GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 in Human [ChEMBL: CHEMBL4523640] [GtoPdb: 414, 411, 407] [UniProtKB: P18507, P47870, P48169]
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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 in Human [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870]
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BGT1/Betaine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3715] [GtoPdb: 932] [UniProtKB: P48065]
ChEMBL Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.41 pIC50 39000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human GABA transporter (hBGT-1) activity. B 4.44 pIC50 36000 nM IC50 J Med Chem (1994) 37: 2334-2342 [PMID:8057281]
ChEMBL Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.56 pIC50 27542.29 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.6 pIC50 25000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.75 pIC50 17782.79 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I386F mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.77 pIC50 17000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 K317R mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.77 pIC50 17000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 K317R mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.79 pIC50 16218.1 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S353A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.8 pIC50 16000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S353A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.82 pIC50 15135.61 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I386F mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.85 pIC50 14125.38 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S381A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.88 pIC50 13182.57 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S381A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.89 pIC50 13000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Q378P mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.96 pIC50 11000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.96 pIC50 11000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453S mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.96 pIC50 11000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453S mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.97 pIC50 10715.19 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.99 pIC50 10232.93 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method B 5 pIC50 10000 nM IC50 J Med Chem (2019) 62: 5797-5809 [PMID:31117514]
ChEMBL Inhibition of human BGT1 Q378P mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.02 pIC50 9549.93 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Q346Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 V337I mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S345A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F324C mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.1 pIC50 8000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 C382T mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.1 pIC50 8000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Q346Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.1 pIC50 7943.28 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 S345A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.1 pIC50 7943.28 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F324C mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.12 pIC50 7585.78 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 C382T mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.13 pIC50 7413.1 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I340V mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.15 pIC50 7000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 V337I mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.18 pIC50 6606.93 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 A328G mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.22 pIC50 6000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F367Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.22 pIC50 6000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I386M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.22 pIC50 6000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I386M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.26 pIC50 5495.41 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 A328G mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.26 pIC50 5495.41 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 I340V mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.27 pIC50 5370.32 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F367Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.29 pIC50 5128.61 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 H312N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.3 pIC50 5000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 H312N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.38 pIC50 4168.69 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F295Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.4 pIC50 4000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 A321M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.4 pIC50 4000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 F295Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.4 pIC50 3981.07 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.41 pIC50 3890.45 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 A321M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.44 pIC50 3630.78 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453S/Y454A double mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.48 pIC50 3311.31 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 V336A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.52 pIC50 3000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Y453S/Y454A double mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.52 pIC50 3000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 V336A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.66 pIC50 2187.76 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 K310N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.7 pIC50 2000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 K310N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.81 pIC50 1548.82 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Q299L mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 6 pIC50 1000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 Q299L mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 6.07 pIC50 851.14 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor α6 subunit/GABA-A receptor; agonist GABA site in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109244] [GtoPdb: 404, 410, 412, 408, 406, 405, 411, 407, 409] [UniProtKB: P14867, P18505, P28472, P31644, P34903, P47869, P47870, P48169, Q16445]
ChEMBL Agonist activity at human alpha-1-beta-2-gamma-2L GABAA receptor expressed in Xenopus oocytes assessed as inhibition of current production by two electrode voltage clamp method F 4.68 pEC50 21100 nM EC50 J Med Chem (2008) 51: 3825-3840 [PMID:18528996]
ChEMBL Agonist activity at GABAA receptor (unknown origin) B 4.78 pEC50 16500 nM EC50 ACS Med Chem Lett (2013) 4: 402-407 [PMID:24900684]
ChEMBL Agonist activity at human alpha1beta2gamma2L GABAA receptor expressed in Xenopus oocytes assessed as potentiation of channel current response by two-electrode voltage clamp electrophysiology assay