Compound name
RGX-104
Protein family
Nuclear Receptors
Target name
NR1H2
Affinity on-target cellular (nM)
3032
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001482aCl
SMILES
C[C@H](CCOc1cccc(CC(=O)O)c1)N(Cc1cccc(C(F)(F)F)c1Cl)CC(c1ccccc1)c1ccccc1.Cl
InChIKey
LCMIYQOJZLRHTO-GJFSDDNBSA-N
NCBI gene ID
7376
UniProt ID
P55055
Synonyms
NER, NER-I, RIP15, LXR-b, LXRb
Mode of action
Agonist
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-hLXR?-LBD or -hLXR?-LBD expression plasmid)
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
20
Selectivity remarks
Screened at 1 µM against NR1H4, NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 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: ?Tm(FGFR3) = 2.11, all other bromodomains and kinases ?Tm < 2 K
Selectivity Number of Off-targets
1