CGP 44532 [Ligand Id: 1082] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL113348
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  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
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  • GABAB receptor in Rat [GtoPdb: 242]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241240] [UniProtKB: O88871Q9Z0U4]
ChEMBL Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex B 6.82 pIC50 152 nM IC50 J Med Chem (1995) 38: 3297-3312 [PMID:7650684]
GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
ChEMBL Antagonist activity at human recombinant GABAc rho1 receptor expressed in Xenopus laevis oocytes at -60mV by two-electrode voltage clamp method F 5.27 pIC50 5400 nM IC50 Bioorg Med Chem Lett (2008) 18: 402-404 [PMID:17981464]
GABAB receptor in Rat [GtoPdb: 242]
GtoPdb - - 8.6 pIC50 - - - Chemistry of GABAB modulators.. The GABA Receptors (1997)

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]