ORIC-101 [Ligand Id: 13167] 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: CHEMBL4161754 |
|---|
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 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 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]
