Compound name
GW9578
Protein family
Nuclear Receptors
Target name
NR1C3
Affinity on-target cellular (nM)
1000
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001142a
SMILES
CCCCCCCN(CCc1ccc(cc1)SC(C)(C)C(=O)O)C(=O)Nc1ccc(F)cc1F
InChIKey
KYQNYMXQHLMADB-UHFFFAOYSA-N
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Reporter gene assay (CV-1 cells were cotransfected with aP2-tk-CAT reporter plasmid, pCH110-?-galactosidase control plasmid and pSG5-Gal4-PPAR? or -PPAR? expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm9903601
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 1 µM against NR1C2, 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 = 20.12 (NR1C2), EC50 = 1400 nM (NR1C2) reported in literature ; 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 Source Knowledge
https://doi.org/10.1021/jm9903601
Selectivity Number of Off-targets
1