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Assay Detail

CHEMBL1069507

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Binding
Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
4
Total Activities
4
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 Autocuration

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.
Saha P, Hödl C, Strauss WS, Steiner R, Goessler W, Kunert O, Leitner A, Haslinger E, Schramm HW.
Bioorg Med Chem (2010) 18 : 1891 -1898
PubMed 20149664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.23 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 10.30
CHEMBL1608 DESMETHYLMIFEPRISTONE 1 9.77
CHEMBL452860 1 9.36
CHEMBL453382 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.05 nM 10.30
CHEMBL1608 DESMETHYLMIFEPRISTONE IC50 = 0.17 nM 9.77
CHEMBL452860 IC50 = 0.44 nM 9.36
CHEMBL453382 IC50 = 34.0 nM 7.47