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Assay Detail

CHEMBL729163

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

Functional
Antagonist activity against the Mineralocorticoid Receptor (MR)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
Zhang P, Terefenko EA, Fensome A, Wrobel J, Winneker R, Lundeen S, Marschke KB, Zhang Z.
J Med Chem (2002) 45 : 4379 -4382
PubMed 12238914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.69 5.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139749 1 5.86
CHEMBL136322 1 5.62
CHEMBL343306 1 5.60
CHEMBL1276308 MIFEPRISTONE 4.0 1 -
CHEMBL138059 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139749 IC50 = 1386.0 nM 5.86
CHEMBL136322 IC50 = 2369.0 nM 5.62
CHEMBL343306 IC50 = 2492.0 nM 5.60
CHEMBL1276308 MIFEPRISTONE IC50 > 1000.0 nM -
CHEMBL138059 IC50 > 10000.0 nM -