dazucorilant [Ligand Id: 13264] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3734774 (Cort113176, CORT-113176, CORT113176, Dazucorilant)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 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 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]