relacorilant [Ligand Id: 13830] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4068611 (Cort 125134, Cort-125134, CORT125134, Relacorilant) |
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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 | Antagonist activity at glucocorticoid receptor in human primary hepatocytes assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs | B | 7.09 | pKi | 81.2 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| GtoPdb | Antagonism of dexamethasone-induced tyrosine amino transferase activity in human HepG2 cells | - | 8.14 | pKi | 7.2 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| 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 | 8.14 | pKi | 7.2 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| Glucocorticoid receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105966] [UniProtKB: A0A8C0QLS2] | ||||||||
| ChEMBL | Antagonist activity at dog glucocorticoid receptor in primary hepatocytes assessed as dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| ChEMBL | Agonist activity at dog glucocorticoid receptor in primary hepatocytes assessed as induction of tyrosine amino transferase activity measured after 20 hrs | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Antagonist activity at rat glucocorticoid receptor in primary hepatocytes assessed as 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] |
| ChEMBL | Agonist activity at rat glucocorticoid receptor in primary hepatocytes assessed as induction of tyrosine amino transferase activity measured after 20 hrs | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
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]
