Compound name
SR8278
Protein family
Nuclear Receptors
Target name
NR1D1
Affinity on-target cellular (nM)
470
CG-Set
Nuclear Receptor set
Recommended Concentration
10 µM
Compound EUbOPEN ID
EUB0001153a
SMILES
O=C(OCC)C1N(C(C2=CC=C(SC)S2)=O)CC3=CC=CC=C3C1
InChIKey
UIEBLUZPSFAFOC-UHFFFAOYSA-N
NCBI gene ID
9572
UniProt ID
P20393
Synonyms
ear-1, hRev, Rev-ErbAalpha, THRA1, REVERBA, REVERBalpha
Mode of action
Antagonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 reporter gene assay (HEK293 cells)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/cb1002575
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
19
Selectivity remarks
Screened at 10 µM against 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): fold-activation = 2.04 (NR4A1); 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)
Selectivity Number of Off-targets
1