AG 1024 [Ligand Id: 5912] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2218926
  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
ChEMBL Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis B 7.11 pKi 77 nM Ki Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
ChEMBL Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay B 5.74 pIC50 1800 nM IC50 Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL IGF1R diphosphorilated was immobilized on a Biacore CM5 chip at 25 degrees C with 2uM K04355 and a flow rate of 30 uL/min using amine coupling at pH 4.50 according to Biacore standard protocol. Data sets were processed and analyzed using the software Biacore 4000 Evaluation. Solvent corrected and double-referenced association and dissociation phase data were fitted to a simple 1:1 interaction model with mass transport limitations B 7.15 pKd 70.75 nM Kd K4DD drug target binding kinetics data
GtoPdb - - 4.74 pIC50 18000 nM IC50 Endocrinology (1997) 138: 1427-33 [PMID:9075698]

ChEMBL data shown on this page come from version 28:

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