Compound name
Andarine
Protein family
Nuclear Receptors
Target name
NR3C4
Affinity biochemical (nM)
4
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002151a
SMILES
CC(=O)NC1=CC=C(C=C1)OC[C@@](C)(C(=O)NC2=CC(=C(C=C2)[N+](=O)[O-])C(F)(F)F)O
InChIKey
YVXVTLGIDOACBJ-SFHVURJKSA-N
Mode of action
Agonist
Affinity biochemical definition
Ki
Affinity biochemical assay type
Competitive radiolabled binding assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1124/jpet.102.040840
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: ?Tm(FGFR3) = 2.59 K, all other bromodomains and kinases ?Tm < 2 K
Selectivity Number of Off-targets
1