baclofen [Ligand Id: 1084] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL701 (BA-34647, BA-34,647, Baclofen, Baclospas-10, Fleqsuvy, Gablofen, Kemstro, Lioresal, Lioresal intrath, Lyflex, Lyvispah, NSC-755906, Ozobax, (rs)-baclofen)
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
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  • GABAB receptor in Human [GtoPdb: 242]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
ChEMBL Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method B 4 pEC50 >100000 nM EC50 J Med Chem (2013) 56: 2456-2465 [PMID:23428109]
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]GABA from Gamma-aminobutyric acid A (GABA-A) receptor in rat brain membranes B 7.52 pIC50 30 nM IC50 J Med Chem (1985) 28: 1440-1446 [PMID:2995665]
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4]
ChEMBL Displacement of [3H]baclofen from gamma-aminobutyric-acid B receptor B 6.38 pIC50 420 nM IC50 J Med Chem (1991) 34: 1307-1313 [PMID:1849996]
ChEMBL Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. B 6.48 pIC50 330 nM IC50 J Med Chem (1991) 34: 2557-2560 [PMID:1652022]
ChEMBL Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutes B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (1996) 6: 1709-1714
ChEMBL Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes B 6.7 pIC50 200 nM IC50 J Med Chem (1987) 30: 743-746 [PMID:3031294]
ChEMBL Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. B 6.74 pIC50 180 nM IC50 J Med Chem (1991) 34: 2557-2560 [PMID:1652022]
ChEMBL Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex B 6.97 pIC50 107 nM IC50 J Med Chem (1995) 38: 3297-3312 [PMID:7650684]
ChEMBL Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranes B 7.22 pIC50 60 nM IC50 J Med Chem (1985) 28: 1440-1446 [PMID:2995665]
ChEMBL In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (1993) 3: 515-518
GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5]
ChEMBL Displacement of [3H]CGP54626 from GABA-B receptor (unknown origin) by radioligand binding assay B 5.22 pKi 6000 nM Ki J Med Chem (2015) 58: 6336-6347 [PMID:25856547]
ChEMBL Percent inhibition against GABA-B receptor at 1 uM B 7.3 pIC50 50 nM IC50 J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum B 7.46 pIC50 35 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 5.77 pEC50 1700 nM EC50 J Med Chem (2013) 56: 2456-2465 [PMID:23428109]
GABAB receptor in Human [GtoPdb: 242]
GtoPdb - - 6.2 pKi - - - Br J Pharmacol (2000) 131: 1050-4 [PMID:11082110];
Biochem Pharmacol (2003) 65: 1103-13 [PMID:12663046]

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]