Compound name
GW7647
Protein family
Nuclear Receptors
Target name
NR1C1
Affinity on-target cellular (nM)
6
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000185b
SMILES
CC(C)(C(=O)O)SC1=CC=C(C=C1)CCN(CCCCC2CCCCC2)C(=O)NC3CCCCC3
InChIKey
PKNYXWMTHFMHKD-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/10.1016/S0960-894X(01)00188-3
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 (NR1C2) = 19.2, EC50 = 6200 nM for 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/10.1016/S0960-894X(01)00188-3
Selectivity Number of Off-targets
1