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: 404414411] [UniProtKB: P14867P18507P47870]
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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: 414405411] [UniProtKB: P18507P47869P47870]
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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: 414412405] [UniProtKB: P18507P28472P47869]
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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: 414406411] [UniProtKB: P18507P34903P47870]
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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: 414412406] [UniProtKB: P18507P28472P34903]
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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: 414412408] [UniProtKB: P18507P28472P31644]
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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: 414412409] [UniProtKB: P18507P28472Q16445]
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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: 404414411] [UniProtKB: P14867P18507P47870]
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: 414405411] [UniProtKB: P18507P47869P47870]
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: 414412405] [UniProtKB: P18507P28472P47869]
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: 414406411] [UniProtKB: P18507P34903P47870]
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: 414412406] [UniProtKB: P18507P28472P34903]
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: 414412408] [UniProtKB: P18507P28472P31644]
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: 414412409] [UniProtKB: P18507P28472Q16445]
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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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: 241240] [UniProtKB: O88871Q9Z0U4]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]