Compound name
SR2211
Protein family
Nuclear Receptors
Target name
NR1F3
Affinity on-target cellular (nM)
320
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001160a
SMILES
FC(C=C1C(C(F)(F)F)(C(F)(F)F)O)=C(C=C1)C(C=C2)=CC=C2CN(CC3)CCN3CC4=CC=NC=C4
InChIKey
KVHKWAZUPPBMLL-UHFFFAOYSA-N
Mode of action
Inverse Agonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 reporter gene assay (HEK293T cells were cotransfected with UAS-luciferase reporter plasmid and Gal4-ROR? expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/cb200496y
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): 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)