[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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
