Compound name
T0901317
Protein family
Nuclear Receptors
Target name
NR1H3
Affinity on-target cellular (nM)
370
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000040b
SMILES
C1=CC=C(C=C1)S(=O)(=O)N(CC(F)(F)F)C2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O
InChIKey
SGIWFELWJPNFDH-UHFFFAOYSA-N
NCBI gene ID
10062
UniProt ID
Q13133
Synonyms
LXR-a, RLD-1, LXRa
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Gal4 reporter gene assay
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm401901d
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel, literature
Selectivity platform number of targets
26
Selectivity remarks
Screened at 1 µM against NR1F1, NR1F2, NR1H4, NR1I1, 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 (NR1H4) = 10.92, EC50 = 1300 nM for NR1H4 reported in literature; 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 Source Knowledge
https://doi.org/10.1021/jm401901d
Selectivity Number of Off-targets
1