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Assay Detail

CHEMBL876979

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Binding
Inhibition of human progesterone receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Fensome A, Bender R, Chopra R, Cohen J, Collins MA, Hudak V, Malakian K, Lockhead S, Olland A, Svenson K, Terefenko EA, Unwalla RJ, Wilhelm JM, Wolfrom S, Zhu Y, Zhang Z, Zhang P, Winneker RC, Wrobel J.
J Med Chem (2005) 48 : 5092 -5095
PubMed 16078826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.47 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138059 1 8.10
CHEMBL136721 1 7.82
CHEMBL136806 1 7.52
CHEMBL117965 1 7.18
CHEMBL329631 1 7.14
CHEMBL315445 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138059 IC50 = 8.0 nM 8.10
CHEMBL136721 IC50 = 15.0 nM 7.82
CHEMBL136806 IC50 = 30.0 nM 7.52
CHEMBL117965 IC50 = 66.0 nM 7.18
CHEMBL329631 IC50 = 73.0 nM 7.14
CHEMBL315445 IC50 = 84.0 nM 7.08