Compound name
Mifepristone
Protein family
Nuclear Receptors
Target name
NR3C3
Affinity on-target cellular (nM)
0.18
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0002157a
SMILES
CC#C[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)O
InChIKey
VKHAHZOOUSRJNA-GCNJZUOMSA-N
Mode of action
Antagonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Reporter gene assay (CV-1 cells)
Affinity on-target cellular source knowledge
https://doi.org/10.1016/S0960-894X(03)00256-7
https://doi.org/10.1016/j.bmc.2008.05.018
https://doi.org/10.1021/jm950747d
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel, literature
Selectivity platform number of targets
23
Selectivity remarks
Screened at 3 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): fold-activation = 7.41 (NR1C3); 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); IC50 = 5000 nM (NR3A2), 1500 nM (CYP2C8), 4900 nM (CYP2C9), 9500 nM (CYP3A4) and 2020 nM (BSEP) reported in literature
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmc.2008.05.018
https://doi.org/10.1021/acs.jmedchem.8b00743
https://doi.org/10.1093/toxsci/kft176
Selectivity Number of Off-targets
6