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Assay Detail

CHEMBL767015

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

Binding
Inhibition of [3H]P4 to progesterone receptor (PR) of human T47D breast carcinoma cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.
Zhang P, Terefenko EA, Fensome A, Wrobel J, Winneker R, Zhang Z.
Bioorg Med Chem Lett (2003) 13 : 1313 -1316
PubMed 12657271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.49 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282650 1 8.52
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 7.97
CHEMBL417110 1 7.00
CHEMBL28164 1 7.00
CHEMBL25454 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282650 IC50 = 3.0 nM 8.52
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 10.8 nM 7.97
CHEMBL417110 IC50 = 100.0 nM 7.00
CHEMBL28164 IC50 = 100.0 nM 7.00
CHEMBL25454 IC50 = 114.0 nM 6.94