Compound name
AZD5423
Protein family
Nuclear Receptors
Target name
NR3C1
Affinity biochemical (nM)
0.9
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000578a
SMILES
C[C@@H]([C@@H](C1=CC(=CC=C1)OC)OC2=CC3=C(C=C2)N(N=C3)C4=CC=C(C=C4)F)NC(=O)C(F)(F)F
InChIKey
ZZUKALQMHNSWTK-UHFFFAOYSA-N
NCBI gene ID
2908
UniProt ID
P04150
Synonyms
GR
Mode of action
Agonist
Affinity biochemical definition
EC50
Affinity biochemical assay type
Radiolabled binding assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.7b01215
https://doi.org/10.1111/bcpt.12621
Affinity biochemical relation
0
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
23
Selectivity remarks
Screened at 1 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR4A1, NR5A2 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)