[3H](R)-(-)-baclofen [Ligand Id: 3428] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL301742 (STX-209, Arbaclofen, STX209, Baclofen (r)-form)
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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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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: 241240] [UniProtKB: O88871Q9Z0U4]
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: 241240] [UniProtKB: O75899Q9UBS5]
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 27:

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]