BI 653048 [Ligand Id: 9715] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3358954
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]

ChEMBL data shown on this page come from version 27:

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]