Compound name
GW0742
Protein family
Nuclear Receptors
Target name
NR1C2
Affinity on-target cellular (nM)
1
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000569a
SMILES
CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC(=C(C=C3)C(F)(F)F)F)C)OCC(=O)O
InChIKey
HWVNEWGKWRGSRK-UHFFFAOYSA-N
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
cell-based
Affinity on-target cellular source knowledge
https://doi.org/10.1016/S0960-894X(03)00207-5
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 NR1C1, NR1C3, 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 = 14.62 (NR1C1) and 10.44 (NR1C3), EC50 = 1100 nM (NR1C1) and EC50 = 2000 nM (NR1C3) 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(03)00207-5
Selectivity Number of Off-targets
2