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Assay Detail

CHEMBL965384

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

Binding
Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells
37
Total Activities
37
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

7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Zhang P, Kern JC, Terefenko EA, Fensome A, Unwalla R, Zhang Z, Cohen J, Berrodin TJ, Yudt MR, Winneker RC, Wrobel J.
Bioorg Med Chem (2008) 16 : 6589 -6600
PubMed 18504132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.27 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.70
CHEMBL501080 1 7.93
CHEMBL117518 1 7.89
CHEMBL487116 1 7.88
CHEMBL486709 1 7.83
CHEMBL487727 1 7.82
CHEMBL488758 1 7.80
CHEMBL487117 1 7.65
CHEMBL487728 1 7.60
CHEMBL486498 1 7.58
CHEMBL519581 1 7.54
CHEMBL530108 1 7.53
CHEMBL488558 1 7.52
CHEMBL529665 1 7.52
CHEMBL486915 1 7.52
CHEMBL530109 1 7.47
CHEMBL487729 1 7.46
CHEMBL506297 1 7.23
CHEMBL486499 1 7.21
CHEMBL520223 1 7.20
CHEMBL519883 1 7.19
CHEMBL487930 1 7.18
CHEMBL488560 1 7.11
CHEMBL488559 1 7.08
CHEMBL527871 1 7.06
CHEMBL486910 1 7.00
CHEMBL519394 1 7.00
CHEMBL486433 1 6.98
CHEMBL486916 1 6.97
CHEMBL488556 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.2 nM 9.70
CHEMBL501080 IC50 = 11.8 nM 7.93
CHEMBL117518 IC50 = 13.0 nM 7.89
CHEMBL487116 IC50 = 13.3 nM 7.88
CHEMBL486709 IC50 = 14.9 nM 7.83
CHEMBL487727 IC50 = 15.0 nM 7.82
CHEMBL488758 IC50 = 15.7 nM 7.80
CHEMBL487117 IC50 = 22.5 nM 7.65
CHEMBL487728 IC50 = 25.0 nM 7.60
CHEMBL486498 IC50 = 26.6 nM 7.58
CHEMBL519581 IC50 = 29.1 nM 7.54
CHEMBL530108 IC50 = 29.3 nM 7.53
CHEMBL488558 IC50 = 30.0 nM 7.52
CHEMBL529665 IC50 = 30.1 nM 7.52
CHEMBL486915 IC50 = 29.9 nM 7.52
CHEMBL530109 IC50 = 34.1 nM 7.47
CHEMBL487729 IC50 = 34.6 nM 7.46
CHEMBL506297 IC50 = 59.2 nM 7.23
CHEMBL486499 IC50 = 62.1 nM 7.21
CHEMBL520223 IC50 = 62.5 nM 7.20
CHEMBL519883 IC50 = 65.2 nM 7.19
CHEMBL487930 IC50 = 65.5 nM 7.18
CHEMBL488560 IC50 = 78.2 nM 7.11
CHEMBL488559 IC50 = 82.4 nM 7.08
CHEMBL527871 IC50 = 88.0 nM 7.06
CHEMBL486910 IC50 = 100.0 nM 7.00
CHEMBL519394 IC50 = 100.0 nM 7.00
CHEMBL486433 IC50 = 104.7 nM 6.98
CHEMBL486916 IC50 = 107.6 nM 6.97
CHEMBL488556 IC50 = 116.7 nM 6.93
CHEMBL530107 IC50 = 138.3 nM 6.86
CHEMBL520534 IC50 = 207.7 nM 6.68
CHEMBL486707 IC50 = 349.4 nM 6.46
CHEMBL488351 IC50 = 365.7 nM 6.44
CHEMBL519560 IC50 = 676.7 nM 6.17
CHEMBL488557 IC50 = 1000.0 nM 6.00
CHEMBL521049 IC50 = 1000.0 nM 6.00