(-)-baclofen [Ligand Id: 1064] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL301742 (Arbaclofen, Baclofen, (r)-, Baclofen, r(-)-, Baclofen, r-, Baclofen (r)-form, D-baclofen, (r)-baclofen, R-(-)-baclofen, STX-209, STX209) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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]muscimol binding to Gamma-aminobutyric acid A (GABA-A) receptor of rat brain membranes | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 2053-2059 [PMID:10354414] |
| GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Nature (1997) 386: 239-46 [PMID:9069281] |
| ChEMBL | Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1999) 42: 2053-2059 [PMID:10354414] |
| ChEMBL | Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5] | ||||||||
| ChEMBL | Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| ChEMBL | Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2013) 56: 2456-2465 [PMID:23428109] |
| GABAB2/GABAB1 in Rat [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Nature (1997) 386: 239-46 [PMID:9069281] |
| GABAB receptor in Rat [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - | Chemistry of GABAB modulators.. The GABA Receptors (1997) |
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]
