[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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| 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] |
| ChEMBL | Substrate uptake by the Sodium- and Chloride-Dependent BetaineTransporter (BGT-1, SLC6A12) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC6A12 cells (PubChem AID: 1794822) | F | 4.44 | pEC50 | 36000 | nM | EC50 | Membrane potential based assay for SLC6A12 using HEK-293 SLC6A12 OE cells |
| 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 GABA-A receptor in rat brain homogenate incubated for 10 mins by microbeta liquid scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Eur J Med Chem (2023) 247: 115071-115071 [PMID:36603509] |
| 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] | ||||||||
| 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] |
| 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] |
| 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] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
