[3H]muscimol [Ligand Id: 4090] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL273481 (Agarin, Muscimol, NSC-333569, Pantherine) |
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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: 404, 410, 412, 408, 406, 405, 411, 407, 409] [UniProtKB: P14867, P18505, P28472, P31644, P34903, P47869, P47870, P48169, Q16445] | ||||||||
| 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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
| 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: 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 | 6.39 | 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: 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 | 6.67 | 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: 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 | 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: 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]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 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]
