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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) |
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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 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]