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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |