Compound name
MS184
Protein family
Nuclear Receptors
Target name
NR4A2
Affinity biochemical (nM)
170
Affinity on-target cellular (nM)
90
CG-Set
Nuclear Receptor set
Recommended Concentration
0,3 µM
Compound EUbOPEN ID
EUB0003338a
SMILES
ClC1=CC=CN2C1=NC(C)=C2NC(C3=CC=C(C4=CC=C(N(C)C)C=C4)O3)=O
InChIKey
HGXSOLYLDMLDRI-UHFFFAOYSA-N
NCBI gene ID
4929
UniProt ID
P43354
Synonyms
TINUR, NOT, RNR1, HZF-3
Mode of action
Agonist
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC (NR4A2)
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/s42004-024-01224-0
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/10.1038/s42004-024-01224-0
Affinity on-target cellular relation
0
Selectivity remarks
Screened at 0.3 µM and 3 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1F3, NR1H3, NR1H4, NR1I1, 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): clean selectivty profile with no significant agonism/antagonism
Selectivity Source Knowledge
https://doi.org/10.1038/s42004-024-01224-0