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 Competitive displacement of 3[H]retinol from biotinylated RBP4 (unknown origin) by surface plasmon resonance analysis B 7.82 pIC50 15 nM IC50 J Med Chem (2019) 62: 5470-5500 [PMID:31079449]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]