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ChEMBL ligand: CHEMBL3734774 |
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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 | Antagonist activity at glucocorticoid receptor in human primary hepatocytes assessed as inhibition of glucocorticoid-induced TAT activity | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
ChEMBL | Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of glucocorticoid-induced TAT activity after 24 hrs | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
ChEMBL | Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
GtoPdb | Determined in a glucocorticoid receptor competitor fluorescence polarization- displacing fluormone GS Red. | - | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
ChEMBL | Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assay | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
ChEMBL | Binding affinity to human recombinant glucocorticoid receptor by fluorescence polarization assay | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
ChEMBL | Antagonist activity at glucocorticoid receptor in rat primary hepatocytes assessed as inhibition of glucocorticoid-induced TAT activity | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
ChEMBL | Agonist activity at glucocorticoid receptor in rat primary hepatocytes assessed as inhibition of glucocorticoid-induced TAT activity | B | 6.55 | pEC50 | 280 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG by patch clamp technique | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5720-5725 [PMID:26546213] |
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]