Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4008021

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at GAL4-fused human PR LBD (680 to 933 residues) expressed in CHO-K1 cells assessed as inhibition of progesterone-induced transactivation activity after 5 to 6 hrs by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Martín-Martínez M, Pérez-Gordillo FL, Álvarez de la Rosa D, Rodríguez Y, Gerona-Navarro G, González-Muñiz R, Zhou MM.
J Med Chem (2017) 60 : 2629 -2650
PubMed 28051871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.33 5.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4096901 1 5.38
CHEMBL4068008 1 5.27
CHEMBL2181927 FINERENONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4096901 IC50 = 4200.0 nM 5.38
CHEMBL4068008 IC50 = 5400.0 nM 5.27
CHEMBL2181927 FINERENONE IC50 >= 10000.0 nM -