GABA [Ligand Id: 1067] 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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| 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 | F | 6 | pEC50 | 990 | nM | EC50 | J Med Chem (2011) 54: 8124-8135 [PMID:22029276] |
| GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507] | ||||||||
| ChEMBL | Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique | F | 4.37 | pEC50 | 43000 | nM | EC50 | J Med Chem (2007) 50: 4147-4161 [PMID:17655213] |
| ChEMBL | Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique | F | 4.37 | pEC50 | 42657.95 | nM | EC50 | J Med Chem (2007) 50: 4147-4161 [PMID:17655213] |
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
| ChEMBL | Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method | B | 1.52 | pEC50 | 1.52 | - | logEC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| ChEMBL | Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A,S343A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method | B | 1.56 | pEC50 | 1.56 | - | logEC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| ChEMBL | Partial agonist activity at GABAAalpha1beta2gamma2s receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as induction of chloride current by two-microelectrode voltage-clamp method | B | 4.29 | pEC50 | 51000 | nM | EC50 | Bioorg Med Chem (2015) 23: 6757-6762 [PMID:26410663] |
| ChEMBL | Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 5.42 | pEC50 | 3801.89 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 5.43 | pEC50 | 3700 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.74 | pEC50 | 1800 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 5.74 | pEC50 | 1800 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.75 | pEC50 | 1778.28 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 5.75 | pEC50 | 1778.28 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138] | ||||||||
| ChEMBL | Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method | B | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2013) 56: 2456-2465 [PMID:23428109] |
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
| ChEMBL | Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytes | F | 4.1 | pEC50 | 80000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870] | ||||||||
| ChEMBL | Agonist activity at human GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.18 | pEC50 | 660.69 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.18 | pEC50 | 660.69 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.19 | pEC50 | 650 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.19 | pEC50 | 650 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869] | ||||||||
| ChEMBL | Agonist activity on human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in Xenopus oocytes | F | 4.4 | pEC50 | 40000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870] | ||||||||
| ChEMBL | Agonist activity at human GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.04 | pEC50 | 920 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.04 | pEC50 | 920 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.04 | pEC50 | 912.01 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.04 | pEC50 | 912.01 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903] | ||||||||
| ChEMBL | Agonist activity on human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in Xenopus oocytes | F | 4.55 | pEC50 | 28000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/GABA A receptor alpha-4/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111366] [GtoPdb: 414, 412, 407] [UniProtKB: P18507, P28472, P48169] | ||||||||
| ChEMBL | Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-4-beta-3-gamma-2 | F | 4.3 | pEC50 | 50000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644] | ||||||||
| ChEMBL | Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 expressed in Xenopus oocytes | F | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445] | ||||||||
| ChEMBL | Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 | F | 5.82 | pEC50 | 1500 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1573-1577 [PMID:11412984] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 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 ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| ChEMBL | Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of human cerebellar cortex preparation | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1980) 23: 702-704 [PMID:7392039] |
| ChEMBL | Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method | B | 7.48 | pKi | 33 | nM | Ki | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations. | F | 5.84 | pIC50 | 1450 | nM | IC50 | J Med Chem (1992) 35: 4092-4097 [PMID:1331456] |
| ChEMBL | Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection. | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (1992) 35: 4092-4097 [PMID:1331456] |
| GABAA receptor α6 subunit/GABAA receptor γ2 subunit/GABAA receptor δ subunit/GABAA receptor α2 subunit/GABAA receptor α3 subunit/GABAA receptor γ3 subunit/GABAA receptor β1 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor π subunit/GABAA receptor α4 subunit/GABAA receptor θ subunit/GABAA receptor γ1 subunit/GABA-A receptor; anion channel in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094133] [GtoPdb: 409, 414, 416, 405, 406, 415, 410, 404, 412, 408, 419, 407, 418, 413] [UniProtKB: A2AMW3, P16305, P22723, P22933, P26048, P26049, P27681, P50571, P62812, P63080, Q8BHJ7, Q8QZW7, Q9D6F4, Q9JLF1, Q9R0Y8] | ||||||||
| ChEMBL | Activation of chloride ion uptake into mouse brain synaptoneurosomes | F | 4.84 | pEC50 | 14300 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1985-1988 [PMID:12113824] |
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2006) 49: 4442-4446 [PMID:16821803] |
| ChEMBL | Displacement of [3H]muscimol from orthosteric binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2019) 62: 2798-2813 [PMID:30763084] |
| ChEMBL | Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of rat ganglion neurons | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (1980) 23: 702-704 [PMID:7392039] |
| ChEMBL | Inhibition of 2 nM [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor in rat brain crude synaptic membranes | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1982) 25: 113-116 [PMID:6276545] |
| ChEMBL | Inhibition of [3H]muscimol binding to GABA-A receptor from rat cortex | B | 6.89 | pIC50 | 128 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| ChEMBL | Inhibition of [3H]muscimol binding to gamma-aminobutyric-acid A (GABA-A) receptor | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1991) 34: 2557-2560 [PMID:1652022] |
| ChEMBL | In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain. | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1983) 26: 895-900 [PMID:6304315] |
| ChEMBL | Inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptosomal membranes | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1982) 25: 1157-1162 [PMID:6292417] |
| ChEMBL | In vitro binding affinity against Gamma-aminobutyric acid A receptor in rat brain synaptic membranes at pH 7.1 | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1990) 33: 71-77 [PMID:2153214] |
| ChEMBL | Inhibition of [3H]GABA binding to gamma-aminobutyric-acid A (GABA-A) receptor | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1991) 34: 1307-1313 [PMID:1849996] |
| ChEMBL | Displacement of [3H]GABA from Gamma-aminobutyric acid A receptor ofrat brain membranes | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1987) 30: 743-746 [PMID:3031294] |
| ChEMBL | Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane at 0.022-0.039 uM | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (1985) 28: 653-660 [PMID:2985785] |
| ChEMBL | In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (1985) 28: 1612-1617 [PMID:2999396] |
| ChEMBL | Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat cerebral cortex | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2006) 49: 5571-5577 [PMID:16942030] |
| ChEMBL | Displacement of [3H]gamma-aminobutyric acid from sodium-independent Gamma-aminobutyric acid (GABA-A) receptor synaptic membrane binding sites from rat brain tissue | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1980) 23: 1142-1144 [PMID:7420361] |
| ChEMBL | Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
| ChEMBL | Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat spinal cord | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2006) 49: 5571-5577 [PMID:16942030] |
| ChEMBL | In vitro inhibition of [3H]THIP binding to Gamma-aminobutyric acid receptor in rat brain synaptic membranes | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1985) 28: 1612-1617 [PMID:2999396] |
| ChEMBL | Inhibition of [3H]GABA binding in GABAA receptor in rat brain synaptic membranes | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2006) 49: 4442-4446 [PMID:16821803] |
| GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Nature (1997) 386: 239-46 [PMID:9069281] |
| ChEMBL | In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 515-518 |
| ChEMBL | Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1991) 34: 2557-2560 [PMID:1652022] |
| ChEMBL | Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1987) 30: 743-746 [PMID:3031294] |
| ChEMBL | In vitro binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptic membranes at pH 7.4 | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1990) 33: 71-77 [PMID:2153214] |
| ChEMBL | Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
| ChEMBL | Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5] | ||||||||
| ChEMBL | Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| ChEMBL | Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay | F | 6.28 | pEC50 | 530 | nM | EC50 | J Med Chem (2013) 56: 2456-2465 [PMID:23428109] |
| GABAB2/GABAB1 in Rat [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Nature (1997) 386: 239-46 [PMID:9069281] |
| GABAB1/GABA-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2064] [GtoPdb: 240] [UniProtKB: Q9UBS5] | ||||||||
| ChEMBL | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method | F | 5.77 | pEC50 | 1700 | nM | EC50 | J Med Chem (2008) 51: 3825-3840 [PMID:18528996] |
| GABAB1 in Rat [GtoPdb: 240] [UniProtKB: Q9Z0U4] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Nature (1997) 386: 239-46 [PMID:9069281] |
| GABAA receptor ρ3 subunit/GABAA receptor ρ1 subunit/GABAA receptor ρ2 subunit/GABA-C receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109242] [GtoPdb: 422, 420, 421] [UniProtKB: A8MPY1, P24046, P28476] | ||||||||
| ChEMBL | Agonist activity against Gamma-aminobutyric acid type C (GABA-C) receptor derived from bovine retinal RNA expressed in Xenopus oocytes | F | 5.77 | pKd | 1700 | nM | Kd | J Med Chem (2000) 43: 1427-1447 [PMID:10780899] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Activity at human GABAA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method | B | 1.5 | pEC50 | 1.5 | - | logEC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813] | ||||||||
| ChEMBL | Activity at rat wild type GABAA alpha-1-beta-2 receptor expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method | B | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2008) 51: 4430-4448 [PMID:18651727] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576] | ||||||||
| ChEMBL | Inhibitory effect was measured for [3H]GABA-uptake from rat synaptosomal membrane | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1986) 29: 125-132 [PMID:3941406] |
| GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574] | ||||||||
| ChEMBL | In vitro inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1985) 28: 1612-1617 [PMID:2999396] |
| GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046] | ||||||||
| ChEMBL | Agonist activity at human recombinant GABAc rho1 receptor expressed in Xenopus laevis oocytes at -60mV by two-electrode voltage clamp method | F | 5.92 | pEC50 | 1190 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 402-404 [PMID:17981464] |
| ChEMBL | Agonist activity at GABAC rho1 receptor (unknown origin) | B | 6 | pEC50 | 1000 | nM | EC50 | ACS Med Chem Lett (2013) 4: 402-407 [PMID:24900684] |
| ChEMBL | Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method | F | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2008) 51: 3825-3840 [PMID:18528996] |
| ChEMBL | Agonist activity at recombinant human GABA-A rho-1 receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at recombinant human GABA-A rho-1 receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 6.47 | pEC50 | 338.84 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.57 | pEC50 | 270 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA rho1 receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.57 | pEC50 | 270 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 6.57 | pEC50 | 269.15 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
| ChEMBL | Agonist activity at human GABAA rho1 receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 6.57 | pEC50 | 269.15 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| GAT1/GABA transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531] | ||||||||
| ChEMBL | Inhibition of human GAT1 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 | Inhibitory activity against human GABA transporter-1 (hGAT1) | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1994) 37: 2334-2342 [PMID:8057281] |
| ChEMBL | Inhibition of human GAT1 expressed in COS cells assessed as decrease in [3H]GABA uptake after 10 mins by scintillation counting analysis | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661] |
| ChEMBL | Inhibition of human GAT1 expresses 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 GAT1 expresses 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] |
| GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648] | ||||||||
| ChEMBL | Inhibition of mouse GTA 1 receptor | B | 4.52 | pIC50 | 30199.52 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| ChEMBL | Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Bioorg Med Chem (2019) 27: 2753-2763 [PMID:31097402] |
| ChEMBL | Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis | B | 5.3 | pIC50 | 5011.87 | nM | IC50 | J Med Chem (2013) 56: 1323-1340 [PMID:23336362] |
| ChEMBL | Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2013) 56: 1323-1340 [PMID:23336362] |
| GAT1/GABA transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978] | ||||||||
| ChEMBL | H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.54 | pIC50 | 2880 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound | B | 5.54 | pIC50 | 2880 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.56 | pIC50 | 2750 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.56 | pIC50 | 2730 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound | B | 5.58 | pIC50 | 2640 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.67 | pIC50 | 2150 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.67 | pIC50 | 2120 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound | B | 5.71 | pIC50 | 1970 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.74 | pIC50 | 1830 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined | B | 5.75 | pIC50 | 1790 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| ChEMBL | H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound | B | 5.79 | pIC50 | 1620 | nM | IC50 | J Med Chem (2004) 47: 5620-5629 [PMID:15509161] |
| GAT2/GABA transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4535] [GtoPdb: 930] [UniProtKB: Q9NSD5] | ||||||||
| ChEMBL | Inhibition of human GAT2 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method | B | 4.59 | pIC50 | 26000 | nM | IC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| GAT2/GABA transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4889] [GtoPdb: 930] [UniProtKB: P31646] | ||||||||
| ChEMBL | Inhibitory activity against rat GABA transporter-2 (rGAT2) | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1994) 37: 2334-2342 [PMID:8057281] |
| GAT3/GABA transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5208] [GtoPdb: 931] [UniProtKB: P48066] | ||||||||
| ChEMBL | Inhibition of human GAT3 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Inhibitory activity against human sodium and chloride dependent GABA transporter 3 | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (1994) 37: 2334-2342 [PMID:8057281] |
| ChEMBL | Inhibition of human GAT3 L314Q mutant expresses 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 GAT3 L314Q mutant expresses 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 GAT3 S468Y mutant expresses 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 GAT3 S468Y mutant expresses 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] |
| GAT2/GABA transporter 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5205] [GtoPdb: 930] [UniProtKB: P31649] | ||||||||
| ChEMBL | Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells | B | 4.56 | pIC50 | 27542.29 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| ChEMBL | Inhibition of mouse GAT2 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis | B | 4.56 | pIC50 | 27542.29 | nM | IC50 | Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250] |
| ChEMBL | Inhibition of mouse GTA 3 receptor | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| GAT3/GABA transporter 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650] | ||||||||
| ChEMBL | Inhibition of mouse GTA4 receptor | B | 4.48 | pIC50 | 33113.11 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis | B | 4.94 | pIC50 | 11481.54 | nM | IC50 | Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250] |
| ChEMBL | Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells | B | 5.09 | pIC50 | 8128.31 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| GABAA receptor β3 subunit/GABAA receptor α3 subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885574] [GtoPdb: 412, 406] [UniProtKB: P28472, P34903] | ||||||||
| ChEMBL | Agonist activity at human GABA type-A alpha3beta3 receptor expressed in xenopus oocytes | B | 5.35 | pEC50 | 4500 | nM | EC50 | Medchemcomm (2016) 7: 426-432 |
| GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABAA receptor θ subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885575] [GtoPdb: 412, 406, 418] [UniProtKB: P28472, P34903, Q9UN88] | ||||||||
| ChEMBL | Agonist activity at human GABA type-A alpha3beta3theta receptor expressed in xenopus oocytes | B | 5.47 | pEC50 | 3400 | nM | EC50 | Medchemcomm (2016) 7: 426-432 |
| 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 (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523640] [GtoPdb: 414, 411, 407] [UniProtKB: P18507, P47870, P48169] | ||||||||
| ChEMBL | Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 5.43 | pEC50 | 3715.35 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 5.43 | pEC50 | 3700 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| 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 (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870] | ||||||||
| ChEMBL | Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 6.63 | pEC50 | 234.42 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| ChEMBL | Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay | B | 6.64 | pEC50 | 230 | nM | EC50 | J Med Chem (2019) 62: 5797-5809 [PMID:31117514] |
| Platelet glycoprotein VI (GPVI) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6] | ||||||||
| ChEMBL | Binding affinity to human platelet lysate GP6 at 0.1 uM by surface plasmon resonance analysis | B | 7.39 | pKd | 41.1 | nM | Kd | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
| Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8] | ||||||||
| ChEMBL | Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting | B | 0.6 | pKi | -0.6 | mM | pKi | Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456] |
| GABAB receptor in Human [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | - | - | - |
Br J Pharmacol (2000) 131: 1050-4 [PMID:11082110]; Biochem Pharmacol (2003) 65: 1103-13 [PMID:12663046] |
| GABAB receptor in Rat [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 8.3 | pIC50 | - | - | - | Chemistry of GABAB modulators.. The GABA Receptors (1997) |
| Glycine Receptor (All subtypes) in Rat [GtoPdb: 428] | ||||||||
| GtoPdb | - | - | 1.2 | pEC50 | - | - | - |
J Physiol (Lond.) (2001) 535: 741-55 [PMID:11559772]; Science (1993) 262: 256-8 [PMID:8211147] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
