muscimol [Ligand Id: 4259] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL273481 (NSC-333569, Muscimol)
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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 [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 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 γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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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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  • GABAA receptor ρ2 subunit/GABA receptor rho-2 subunit in Human [ChEMBL: CHEMBL2375] [GtoPdb: 421] [UniProtKB: P28476]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D-amino-acid oxidase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6172] [UniProtKB: P00371]
ChEMBL Inhibition of pig D-amino acid oxidase B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2008) 51: 3357-3359 [PMID:18507366]
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: 404410412408406405411407409] [UniProtKB: P14867P18505P28472P31644P34903P47869P47870P48169Q16445]
ChEMBL Agonist activity at GABAA receptor (unknown origin) B 4.57 pEC50 27000 nM EC50 ACS Med. Chem. Lett. (2013) 4: 402-407 [PMID:24900684]
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 GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.27 pEC50 540 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 6.27 pEC50 540 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 6.27 pEC50 537.03 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 6.27 pEC50 537.03 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 GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.39 pEC50 410 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 6.39 pEC50 410 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 6.39 pEC50 407.38 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 6.39 pEC50 407.38 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
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 GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.67 pEC50 213.8 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 6.67 pEC50 213.8 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 6.68 pEC50 210 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 6.68 pEC50 210 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
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]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of human cerebellar cortex preparation B 7.96 pKi 11 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 8.22 pKi 6 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 6.87 pIC50 135 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
ChEMBL Percent inhibition against GABAA receptor alpha at a compound concentration of 1 uM B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
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 8.7 pIC50 2 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
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 Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of rat ganglion neurons B 8.4 pKi 4 nM Ki J. Med. Chem. (1980) 23: 702-704 [PMID:7392039]
ChEMBL Displacement of [3H]GABA from Gamma-aminobutyric acid A receptor ofrat brain membranes B 8 pIC50 10 nM IC50 J. Med. Chem. (1987) 30: 743-746 [PMID:3031294]
ChEMBL In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes B 8.22 pIC50 6 nM IC50 J. Med. Chem. (1985) 28: 1612-1617 [PMID:2999396]
ChEMBL Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2000) 43: 4930-4933 [PMID:11150163]
ChEMBL Affinity for GGABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2002) 45: 2454-2468 [PMID:12036354]
ChEMBL In vitro inhibition of [3H]THIP binding to Gamma-aminobutyric acid receptor in rat brain synaptic membranes B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1985) 28: 1612-1617 [PMID:2999396]
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 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (1980) 23: 1142-1144 [PMID:7420361]
ChEMBL Displacement of [3H]- muscimol in cerebral tissue of male rats B 8.52 pIC50 3 nM IC50 J. Med. Chem. (1985) 28: 1109-1111 [PMID:2991521]
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 8.22 pIC50 6 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 Partial agonist activity against human rho-1 subunit GABA-C receptor expressed in Xenopus oocytes F 5.64 pKd 2300 nM Kd J. Med. Chem. (2000) 43: 1427-1447 [PMID:10780899]
ChEMBL Partial agonist activity at GABAC rho1 receptor (unknown origin) B 5.64 pEC50 2300 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 5.85 pEC50 1400 nM EC50 J. Med. Chem. (2008) 51: 3825-3840 [PMID:18528996]
ChEMBL Agonist activity at human GABAA rho1 receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.15 pEC50 700 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 6.15 pEC50 700 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 6.16 pEC50 691.83 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 6.16 pEC50 691.83 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
GABAA receptor ρ2 subunit/GABA receptor rho-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375] [GtoPdb: 421] [UniProtKB: P28476]
ChEMBL Partial agonist activity against human rho-2 subunit GABA-C receptor expressed in Xenopus oocytes F 5.85 pKd 1400 nM Kd J. Med. Chem. (2000) 43: 1427-1447 [PMID:10780899]

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]