Compound name
Fludrocortisone acetate
Protein family
Nuclear Receptors
Target name
NR3C2
Affinity on-target cellular (nM)
0.2
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000561a
SMILES
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@]2([C@H](C[C@]4([C@H]3CC[C@@]4(C(=O)CO)O)C)O)F
InChIKey
SYWHXTATXSMDSB-GSLJADNHSA-N
NCBI gene ID
4306
UniProt ID
P08235
Synonyms
MR
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Reporter gene assay (SK-N-MC cells were cotransfected with MTV-LUC reporter plasmid, pCHll0-SV40 control plasmid and pGEM4-hGR or -hMR expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1016/0922-4106(93)90072-H
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 againstNR1A1, 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)