Compound name
CPD53
Protein family
Nuclear Receptors
Target name
NR4A2
Affinity biochemical (nM)
1000
Affinity on-target cellular (nM)
26000
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
4929
UniProt ID
P43354
Synonyms
TINUR, NOT, RNR1, HZF-3
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