ORIC-101 [Ligand Id: 13167] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4161754 |
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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 GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method | B | 7.6 | pIC50 | 24.9 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method | B | 7.67 | pIC50 | 21.2 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method | B | 7.71 | pIC50 | 19.5 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method | B | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| GtoPdb | Inhibitory potency determined in a GR luciferase antagonist assay. | - | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| Glucocorticoid receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105966] [UniProtKB: A0A8C0QLS2] | ||||||||
| ChEMBL | Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method | B | 7.46 | pIC50 | 34.3 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method | B | 7.61 | pIC50 | 24.5 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| Glucocorticoid receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295956] [UniProtKB: Q9N1U3] | ||||||||
| ChEMBL | Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method | B | 6.74 | pIC50 | 181 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method | B | 7.41 | pIC50 | 39.3 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method | B | 7.23 | pIC50 | 59.4 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method | B | 7.34 | pIC50 | 45.6 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
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]
