Compound name
APAA
Protein family
Nuclear Receptors
Target name
NR1H3
Affinity on-target cellular (nM)
1
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001167a
SMILES
CC(Oc1cc2c(CC[C@H]3[C@](CCC[C@@]32C)(C(OC([C@]4(CCC[C@@]5(c6c(CC[C@@H]45)ccc(OC(C)=O)c6)C)C)=O)=O)C)cc1)=O
InChIKey
OUJQRQRBNRGQTC-SPGSYPTKSA-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 (HEK293 cells were cotransfected with pUAS(5x)-tk-luciferase reporter plasmid, pEGFP-N1 control plasmid and pcDNA3-LXR?/GAL4 or pcDNA3-LXR?/GAL4)
Affinity on-target cellular source knowledge
https://doi.org/10.1074/jbc.M108225201
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: clean selectivity profile with no significant binding (?Tm < 2 K)