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

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ChEMBL ligand: CHEMBL113348
1 CHEMBL113348_lig_chart_1 GABA B receptor Rat
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  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
  • This target only has 0 pki data point
2 CHEMBL113348_lig_chart_2 GABA receptor rho-1 subunit Human
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  • GABAB receptor in Rat [GtoPdb: 242]
  • This target only has 0 pki data point
3 CHEMBL113348_lig_chart_3 GABAB receptor Rat
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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: 241, 240] [UniProtKB: O88871, Q9Z0U4]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]