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Assay Detail

CHEMBL902173

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

Functional
Antagonist activity at progesterone receptor expressed in T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
26
Total Activities
26
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

SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.
Kern JC, Terefenko EA, Fensome A, Unwallla R, Wrobel J, Zhu Y, Cohen J, Winneker R, Zhang Z, Zhang P.
Bioorg Med Chem Lett (2007) 17 : 189 -192
PubMed 17027272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.24 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247902 1 8.30
CHEMBL247053 1 8.09
CHEMBL396908 1 8.08
CHEMBL428210 1 8.05
CHEMBL239792 1 8.04
CHEMBL248101 1 7.88
CHEMBL247054 1 7.84
CHEMBL136721 1 7.82
CHEMBL343306 1 7.64
CHEMBL247295 1 7.56
CHEMBL394306 1 7.53
CHEMBL391361 1 7.52
CHEMBL398801 1 7.49
CHEMBL396093 1 7.43
CHEMBL247499 1 7.38
CHEMBL246885 1 7.26
CHEMBL246884 1 7.25
CHEMBL241732 1 7.18
CHEMBL241733 1 7.14
CHEMBL392848 1 7.00
CHEMBL393641 1 6.69
CHEMBL393642 1 6.00
CHEMBL246886 1 6.00
CHEMBL392704 1 6.00
CHEMBL247090 1 5.52
CHEMBL247089 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247902 IC50 = 5.0 nM 8.30
CHEMBL247053 IC50 = 8.1 nM 8.09
CHEMBL396908 IC50 = 8.4 nM 8.08
CHEMBL428210 IC50 = 9.0 nM 8.05
CHEMBL239792 IC50 = 9.2 nM 8.04
CHEMBL248101 IC50 = 13.1 nM 7.88
CHEMBL247054 IC50 = 14.5 nM 7.84
CHEMBL136721 IC50 = 15.1 nM 7.82
CHEMBL343306 IC50 = 23.0 nM 7.64
CHEMBL247295 IC50 = 27.4 nM 7.56
CHEMBL394306 IC50 = 29.8 nM 7.53
CHEMBL391361 IC50 = 30.0 nM 7.52
CHEMBL398801 IC50 = 32.2 nM 7.49
CHEMBL396093 IC50 = 37.1 nM 7.43
CHEMBL247499 IC50 = 42.2 nM 7.38
CHEMBL246885 IC50 = 54.4 nM 7.26
CHEMBL246884 IC50 = 56.0 nM 7.25
CHEMBL241732 IC50 = 66.1 nM 7.18
CHEMBL241733 IC50 = 71.8 nM 7.14
CHEMBL392848 IC50 = 100.0 nM 7.00
CHEMBL393641 IC50 = 205.8 nM 6.69
CHEMBL393642 IC50 = 1000.0 nM 6.00
CHEMBL246886 IC50 = 1000.0 nM 6.00
CHEMBL392704 IC50 = 1000.0 nM 6.00
CHEMBL247090 IC50 = 3000.0 nM 5.52
CHEMBL247089 IC50 = 3000.0 nM 5.52