A1120 [Ligand Id: 8792] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1230001
  • retinol binding protein 4/Plasma retinol-binding protein in Human [ChEMBL: CHEMBL3100] [GtoPdb: 2549] [UniProtKB: P02753]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
retinol binding protein 4/Plasma retinol-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3100] [GtoPdb: 2549] [UniProtKB: P02753]
ChEMBL Inhibition of retinol-induced interaction of bacterially expressed MBP-tagged RBP4 (unknown origin) with Eu3+ cryptate labeled TTR by HTRF assay B 6.91 pIC50 122 nM IC50 J. Med. Chem. (2015) 58: 5863-5888 [PMID:26181715]
ChEMBL Displacement of [3H]-retinol from human recombinant RBP4 by scintillation proximity assay B 7.05 pIC50 89 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2885-2891 [PMID:24835984]
ChEMBL Displacement of [3H]-retinol from RBP4 (unknown origin) by scintillation proximity assay B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2015) 58: 5863-5888 [PMID:26181715]
ChEMBL Displacement of [3H]retinol from biotinylated human RBP4 by scintillation proximity assay B 7.83 pIC50 14.8 nM IC50 J. Med. Chem. (2014) 57: 7731-7757 [PMID:25210858]
GtoPdb Measured using a FRET assay to monitor human RBP4–transthyretin interaction. - 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2885-91 [PMID:24835984]
ChEMBL Inhibition of human recombinant RBP4-transthyretin interaction by FRET analysis B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2885-2891 [PMID:24835984]
ChEMBL Antagonist activity at maltose binding protein-tagged RBP4 (unknown origin) expressed in Escherichia coli assessed as inhibition of retinol-induced protein/transthyretin interaction by HTRF assay B 9.81 pIC50 0.15 nM IC50 J. Med. Chem. (2014) 57: 7731-7757 [PMID:25210858]

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]