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Assay Detail

CHEMBL924027

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

Functional
Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type T47D
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
Jin C, Manikumar G, Kepler JA, Cook CE, Allan GF, Kiddoe M, Bhattacharjee S, Linton O, Lundeen SG, Sui Z.
Bioorg Med Chem Lett (2007) 17 : 5754 -5757
PubMed 17855092 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.82 10.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 10.27
CHEMBL250220 1 9.47
CHEMBL400582 1 9.23
CHEMBL439234 1 9.20
CHEMBL250425 1 9.01
CHEMBL249426 1 9.00
CHEMBL401267 1 8.34
CHEMBL429114 1 7.75
CHEMBL250221 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.054 nM 10.27
CHEMBL250220 IC50 = 0.34 nM 9.47
CHEMBL400582 IC50 = 0.59 nM 9.23
CHEMBL439234 IC50 = 0.63 nM 9.20
CHEMBL250425 IC50 = 0.98 nM 9.01
CHEMBL249426 IC50 = 1.0 nM 9.00
CHEMBL401267 IC50 = 4.6 nM 8.34
CHEMBL429114 IC50 = 18.0 nM 7.75
CHEMBL250221 IC50 = 82.0 nM 7.09