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ChEMBL ligand: CHEMBL3358954 (Bi 653048) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
ChEMBL | Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
GtoPdb | - | - | 7.15 | pIC50 | 70 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-23 [PMID:25516791] |
ChEMBL | Displacement of RU-486 from GR (unknown origin) by fluorescence polarization assay | B | 7.26 | pIC50 | 55 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-1323 [PMID:25516791] |
ChEMBL | Fluorescence polarization assay | B | 7.26 | pIC50 | 55 | nM | IC50 | Data for DCP probe BI 653048 |
ChEMBL | Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-1323 [PMID:25516791] |
ChEMBL | Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
Glucocorticoid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3144] [GtoPdb: 625] [UniProtKB: P06537] | ||||||||
ChEMBL | Agonist activity at GR in mouse RAW cells assessed as suppression of TNF-alpha-induced IL-6 production | B | 6.22 | pIC50 | 600 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-1323 [PMID:25516791] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG channel expressed in recombinant HEK293 cells by whole cell patch-clamp technique | B | 4.52 | pIC50 | >30000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-1323 [PMID:25516791] |
Interleukin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795129] [UniProtKB: P05231] | ||||||||
ChEMBL | Fibroblast IL-6 assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Data for DCP probe BI 653048 |
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]