Compound name
8-Phenyltheophylline
Protein family
Nuclear Receptors
Target name
NR2E1
Affinity on-target cellular (nM)
500
CG-Set
Nuclear Receptor set
Recommended Concentration
3 µM
Compound EUbOPEN ID
EUB0003344a
SMILES
O=C(C(N1)=C(N2C)N=C1C3=CC=CC=C3)N(C)C2=O
InChIKey
PJFMAVHETLRJHJ-UHFFFAOYSA-N
NCBI gene ID
7101
UniProt ID
Q9Y466
Synonyms
TLL, XTLL
Mode of action
Inverse 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/acsptsci.1c00195
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
2