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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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-)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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: 404410414] [UniProtKB: P14867P18505P18507]
There should be some charts here, you may need to enable JavaScript!
  • 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: 404414411] [UniProtKB: P14867P18507P47870]
  • 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: 414404411] [UniProtKB: P18508P62813P63138]
There should be some charts here, you may need to enable JavaScript!
  • 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: 404414412] [UniProtKB: P14867P18507P28472]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414405411] [UniProtKB: P18507P47869P47870]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414412405] [UniProtKB: P18507P28472P47869]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414406411] [UniProtKB: P18507P34903P47870]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414412406] [UniProtKB: P18507P28472P34903]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414412407] [UniProtKB: P18507P28472P48169]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414412408] [UniProtKB: P18507P28472P31644]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414412409] [UniProtKB: P18507P28472Q16445]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor β3 subunit/GABAA receptor α3 subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 in Human [ChEMBL: CHEMBL3885574] [GtoPdb: 412406] [UniProtKB: P28472P34903]
There should be some charts here, you may need to enable JavaScript!
  • 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: 412406418] [UniProtKB: P28472P34903Q9UN88]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414411407] [UniProtKB: P18507P47870P48169]
There should be some charts here, you may need to enable JavaScript!
  • 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: 414408411] [UniProtKB: P18507P31644P47870]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
There should be some charts here, you may need to enable JavaScript!
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: 404410412408406405411407409] [UniProtKB: P14867P18505P28472P31644P34903P47869P47870P48169Q16445]
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