ZK216348 [Ligand Id: 8643] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL216272 (ZK-216348)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Binding affinity to human recombinant androgen receptor expressed in baculovirus infected Sf9 cells B 6.2 pIC50 630.96 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production B 7.5 pIC50 31.62 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
GtoPdb - - 7.69 pIC50 20.3 nM IC50 Proc Natl Acad Sci USA (2004) 101: 227-32 [PMID:14694204]
ChEMBL Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells B 7.7 pIC50 19.95 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
ChEMBL Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay B 8.2 pIC50 6.31 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
ChEMBL Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay B 8.52 pIC50 3 nM IC50 J Med Chem (2006) 49: 7887-7896 [PMID:17181172]
ChEMBL Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay B 7.9 pEC50 12.59 nM EC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Binding affinity to human recombinant mineralocorticoid receptor expressed in baculovirus infected Sf9 cells B 7.1 pIC50 79.43 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
ChEMBL Inhibition of tetramethylrhodamine labeled dexamethasone binding to MR by FP assay B 7.42 pIC50 38 nM IC50 J Med Chem (2006) 49: 7887-7896 [PMID:17181172]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Binding affinity to human recombinant progesterone receptor expressed in baculovirus infected Sf9 cells B 7.7 pIC50 19.95 nM IC50 Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743]
ChEMBL Inhibition of tetramethylrhodamine labeled RU486 binding to PR by FP assay B 7.72 pIC50 19 nM IC50 J Med Chem (2006) 49: 7887-7896 [PMID:17181172]

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]