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ChEMBL ligand: CHEMBL39071 (Isoguvacine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
ChEMBL | Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 4.95 | pEC50 | 11220.18 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
ChEMBL | Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 4.96 | pEC50 | 11000 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
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 GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.35 | pEC50 | 4500 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
ChEMBL | Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.35 | pEC50 | 4466.84 | 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 | 4.3 | pEC50 | 50000 | 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 GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.25 | pEC50 | 5623.41 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
ChEMBL | Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 5.25 | pEC50 | 5600 | 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 | 4.26 | pEC50 | 55000 | 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 | 4.12 | pEC50 | 75000 | 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 | 4.7 | pEC50 | 20000 | 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]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method | B | 7.26 | pKi | 55 | nM | Ki | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
ChEMBL | Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method | B | 7.26 | pKi | 54.95 | nM | Ki | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
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 | Inhibition of [3H]-GABA binding to GABA-A receptor in rat cerebral cortex homogenates | B | 6.31 | pIC50 | 490 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 247-248 |
ChEMBL | Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
ChEMBL | Effective concentration for stimulation of [3H]diazepam binding to rat cortical membranes | F | 5.51 | pEC50 | 3100 | nM | EC50 | Bioorg Med Chem Lett (1991) 1: 247-248 |
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
ChEMBL | Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
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 GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 4.41 | pEC50 | 39000 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
ChEMBL | Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay | B | 4.41 | pEC50 | 38904.51 | nM | EC50 | Eur J Med Chem (2014) 84: 404-416 [PMID:25038482] |
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 | 0.76 | pKi | -0.76 | mM | pKi | Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456] |
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]