Compound name
Medroxyprogesterone
Protein family
Nuclear Receptors
Target name
NR3C1
Affinity on-target cellular (nM)
10
CG-Set
Nuclear Receptor set
Recommended Concentration
0.3 µM
Compound EUbOPEN ID
EUB0000562a
SMILES
C[C@H]1C[C@@H]2[C@H](CC[C@]3([C@H]2CC[C@@]3(C(=O)C)O)C)[C@@]4(C1=CC(=O)CC4)C
InChIKey
FRQMUZJSZHZSGN-HBNHAYAOSA-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 (CV-1 cells were cotransfected with MTV-LUC reporter plasmid, pRS-?-Gal plasmid and a receptor plasmid contraining hGR, hPR or hAR)
Affinity on-target cellular source knowledge
https://doi.org/10.1021/jm9705768
https://doi.org/10.1021/jm980366a
https://doi.org/10.1021/jm020477g
https://doi.org/10.1016/S0960-894X(98)00608-8
https://doi.org/10.1021/jm980723h
https://doi.org/10.1021/jm9705770
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel, literature
Selectivity platform number of targets
23
Selectivity remarks
Screened at 0.3 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); IC50 = 1800 nM (17?-HSD1), 4100 nM (17?-HSD2), 300 nM (17?-HSD3), 924 nM (NR3A1) and 1197 nM (NR3C2) reported in literature
Selectivity Source Knowledge
https://doi.org/10.1016/j.ejmech.2012.12.045
https://doi.org/10.1021/jm9705768
https://doi.org/10.1021/jm980366a
Selectivity Number of Off-targets
5