Compound name
ME43
Protein family
Nuclear Receptors
Target name
NR4A3
Affinity biochemical (nM)
120
Affinity on-target cellular (nM)
70
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0003337a
SMILES
O=C(Nc1cnc2ccccc2c1)c1cc2[nH]ccc2cc1Cl
InChIKey
ZJPUSKBFLQMYJU-UHFFFAOYSA-N
NCBI gene ID
8013
UniProt ID
Q92570
Synonyms
CSMF, CHN, NOR1, MINOR
Mode of action
Agonist
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC (NR4A2)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.4c03104
Affinity on-target cellular definition
EC50
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.4c03104
Affinity on-target cellular relation
0
Selectivity remarks
Screened at 3 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1H4, NR1I3, NR2A1, NR2B1, 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): EC50 = 1500 nM (NR1I2, binding assay)
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.4c03104
Selectivity Number of Off-targets
2