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ChEMBL ligand: CHEMBL216272 (ZK-216348) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]