Compound name
SR1078
Protein family
Nuclear Receptors
Target name
NR1F3
Affinity on-target cellular (nM)
2000
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001156a
SMILES
O=C(NC1=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C1)C2=CC=C(C(F)(F)F)C=C2
InChIKey
DUXWIYXHHGNUJU-UHFFFAOYSA-N
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Gal4 reporter gene assay (HEK293 cells)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/cb100223d
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 NR1F1, NR1F2, 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): no significant difference between NR1F3 and VP16 activation; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: ?Tm(FGFR3) = 2.93 K; all other bromodomains and kinases ?Tm < 2 K
Selectivity Number of Off-targets
2