apararenone [Ligand Id: 12039] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2181929 (Apararenona, Apararenone, Mt-3995, MT-3995) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Displacement of [3H]-methyltrienolene from human androgen receptor incubated overnight by liquid scintillation counting analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Displacement of [3H]-estradiol from recombinant full-length human estrogen beta receptor expressed in baculovirus infected insect cells incubated overnight by liquid scintillation counting analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Displacement of [3H]-dexamethasone from recombinant full length human glucocorticoid receptor expressed in baculovirus infected insect cells incubated overnight by liquid scintillation counting analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Displacement of [3H]-dexamethasone from rat glucocorticoid receptor incubated overnight by liquid scintillation counting analysis | B | 4.07 | pKi | 84200 | nM | Ki | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| GtoPdb | Binding to hMR | - | 7 | pKi | 100 | nM | Ki | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| ChEMBL | Displacement of [3H]-aldosterone from recombinant human mineralocorticoid receptor expressed in baculovirus infected insect cells incubated overnight by liquid scintillation counting analysis | B | 6.56 | pIC50 | 276 | nM | IC50 | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| ChEMBL | Antagonist activity at human wild-type mineralocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of aldosterone-induced transcriptional activity incubated for 24 hrs in presence of 1 nM aldosterone by Steady-Glo reagent based reporter gene assay | B | 6.59 | pIC50 | 256 | nM | IC50 | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| Mineralocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3507] [GtoPdb: 626] [UniProtKB: P22199] | ||||||||
| ChEMBL | Displacement of [3H]-aldosterone from rat mineralocorticoid receptor incubated overnight by liquid scintillation counting analysis | B | 7.51 | pKi | 30.8 | nM | Ki | J Med Chem (2022) 65: 8127-8143 [PMID:35652647] |
| ChEMBL | Binding affinity to rat mineralocorticoid receptor | B | 6.3 | pIC50 | <500 | nM | IC50 | J Med Chem (2012) 55: 7957-7966 [PMID:22866979] |
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]
