[3H](R)-(-)-baclofen [Ligand Id: 3428] 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, STX209, STX-209)
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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]
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]

ChEMBL data shown on this page come from version 32:

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]