Compound name
CPD53
Protein family
Nuclear Receptors
Target name
NR4A3
Affinity biochemical (nM)
1000
Affinity on-target cellular (nM)
39000
CG-Set
Nuclear Receptor set
Recommended Concentration
50 µM
Compound EUbOPEN ID
EUB0003343a
SMILES
CN(C)C(=O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1
InChIKey
JZMZNOFEMDPCKX-UHFFFAOYSA-N
NCBI gene ID
8013
UniProt ID
Q92570
Synonyms
CSMF, CHN, NOR1, MINOR
Mode of action
Inverse Agonist
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC (NR4A2)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.4c01218
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-hNur77-LBD or pFA-CMV-hNurr1-LBD, or pFA-CMV-hNOR1-LBD expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/acs.jmedchem.4c01218
Affinity on-target cellular relation
0
Selectivity remarks
Screened at 50 µM against NR1A1, NR1B1, NR1,C1, NR1C2, NR1C3, NR1F3, NR1H3, NR1H4, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR2B2, NR2B3, 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)
Selectivity Number of Off-targets
1