Compound name
Mapracorat
Protein family
Nuclear Receptors
Target name
NR3C1
Affinity on-target cellular (nM)
1.6
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0003334a
SMILES
CC1=NC2=C(C=C1)C(=CC=C2)NC[C@](CC(C)(C)C3=CC(=CC4=C3OCC4)F)(C(F)(F)F)O
InChIKey
VJGFOYBQOIPQFY-XMMPIXPASA-N
NCBI gene ID
2908
UniProt ID
P04150
Synonyms
GR
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Reporter gene assay
Affinity on-target cellular source knowledge
https://doi.org/10.1111/j.1476-5381.2009.00238.x
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)