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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 | Affinity Biochemical interaction (Fluorescence polarization assay) EUB0000314b NR3C1 | B | 7.26 | pIC50 | 55 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
ChEMBL | Fluorescence polarization assay | B | 7.26 | pIC50 | 55 | nM | IC50 | Data for DCP probe BI 653048 |
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 | Affinity Phenotypic Cellular interaction (Fibroblast IL-6 assay (inhibition of IL-6 production by human foreskin fibroblasts stimulated by IL-1)) EUB0000314b NR3C1 | F | 7.64 | pIC50 | 23 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
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 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]