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

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ChEMBL ligand: CHEMBL701 (BA-34,647, BA-34647, 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]