Compound name
Oxatomide
Protein family
Nuclear Receptors
Target name
NR1I2
Affinity on-target cellular (nM)
6175
CG-Set
Nuclear Receptor set
Recommended Concentration
10 µM
Compound EUbOPEN ID
EUB0002358a
SMILES
O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1
InChIKey
BAINIUMDFURPJM-UHFFFAOYSA-N
NCBI gene ID
8856
UniProt ID
O75469
Synonyms
ONR1, PXR, BXR, SXR, PAR2
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV-hPXR-LBD expression plasmid)
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel, literature
Selectivity platform number of targets
20
Selectivity remarks
Screened at 10 µM against 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): 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)