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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 |
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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 31:
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]