Compound name
GSK5182
Protein family
Nuclear Receptors
Target name
NR3B3
Affinity on-target cellular (nM)
2700
CG-Set
Nuclear Receptor set
Recommended Concentration
10 µM
Compound EUbOPEN ID
EUB0001912a
SMILES
CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCO)\C2=CC=CC=C2)/C3=CC=C(C=C3)O
InChIKey
ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
Mode of action
Inverse Agonist
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/j.bmc.2017.01.019
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 10 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); IC50 = 320 nM (NR3A1, binding assay)
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmcl.2005.11.030
Selectivity Number of Off-targets
1