Compound name
GFS105
Protein family
Nuclear Receptors
Target name
NR2E1
Affinity on-target cellular (nM)
1000
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0003328a
SMILES
CC1=CN(C=N1)C2=CC(C(F)(F)F)=CC(NC(C3=CC(OCCCC)=NC4=C3C=CC=C4)=O)=C2
InChIKey
RTKBIHCZDFXHLC-UHFFFAOYSA-N
NCBI gene ID
7101
UniProt ID
Q9Y466
Synonyms
TLL, XTLL
Mode of action
Agonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 reporter gene assay
Affinity on-target cellular source knowledge
https://doi.org/10.1021/acs.jmedchem.1c01757
Affinity on-target cellular relation
0
Selectivity remarks
Screened at 3 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, 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
Selectivity Source Knowledge
https://doi.org/10.1021/acsptsci.4c00719
Selectivity Number of Off-targets
3