Compound name
Eplerenone
Protein family
Nuclear Receptors
Target name
NR3C2
Affinity on-target cellular (nM)
122
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002145a
SMILES
C[C@]12CCC(=O)C=C1C[C@H]([C@@H]3[C@]24[C@H](O4)C[C@]5([C@H]3CC[C@@]56CCC(=O)O6)C)C(=O)OC
InChIKey
JUKPWJGBANNWMW-VWBFHTRKSA-N
NCBI gene ID
4306
UniProt ID
P08235
Synonyms
MR
Mode of action
Antagonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 reporter gene assay (HUH7 cells were cotransfected with a luciferase reporter under Gal4 control and Gal4-MR-LBD)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm100506y
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
23
Selectivity remarks
Screened at 1 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR4A1, NR5A2 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)