Compound name
LXR-623
Protein family
Nuclear Receptors
Target name
NR1H2
Affinity on-target cellular (nM)
3670
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0000082b
SMILES
FC(C=C1)=CC=C1C2=C3C(C(C(F)(F)F)=CC=C3)=NN2CC4=CC=C(F)C=C4Cl
InChIKey
KYWWJENKIMRJBI-UHFFFAOYSA-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 reporter gene assay (Huh-7 cells were cotransfected with a Gal4-Luc driven reporter plasmid and Gal4-DBD-hLXR?- or hLXR?-LBD expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm800799q
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel, literature
Selectivity platform number of targets
23
Selectivity remarks
Screened at 3 µM against NR1H4, NR1I1, NR1I2, NR1I3, 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): fold-activation = 2.24 (NR1I2) and 1.82 (NR2E1), EC50 = 1770 nM (NR1I2) in a radiolabled binding assay; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)
Selectivity Number of Off-targets
2