Compound name
GW3965
Protein family
Nuclear Receptors
Target name
NR1H3
Affinity on-target cellular (nM)
190
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0000572aCl
SMILES
C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl
InChIKey
NMPUWJFHNOUNQU-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
repoter gene assay
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm0255116
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 3 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: clean selectivity profile with no significant binding (?Tm < 2 K)