Compound name
DG-172
Protein family
Nuclear Receptors
Target name
NR1C2
Affinity on-target cellular (nM)
1823
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001483aCl
SMILES
CN1CCN(c2ccc(/C=C(\C#N)c3ccccc3Br)cc2)CC1.Cl.Cl
InChIKey
SABUORLIDVBCPI-WTLOABTRSA-N
Mode of action
Antagonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV-hPPAR?-LBD expression plasmid; L-165,041 1 µM used for receptor activation)
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
20
Selectivity remarks
Screened at 1 µM against NR1C3, NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 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)