ZK216348 [Ligand Id: 8643] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
