isoguvacine [Ligand Id: 4226] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL39071 (Isoguvacine)
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]