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Assay Detail

CHEMBL3072496

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

Binding
Inhibition of tissue factor in Homo sapiens (human) THP1-cells using factor 10a chromogenic substrate assessed as inhibition of LPS-iduced procoagulant activity incubated for 1 hr prior to LPS-challenge measured after 5 hr by spectrophotometric analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tissue factor (CHEMBL4081)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structureactivity relationships
Ge H, Chen L, Zhang J, Kou J, Yu B
Med Chem Res (2013) 22 : 3242 -3246
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.57 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17201 1 10.28
CHEMBL276473 4'-HYDROXYCHALCONE 1 9.92
CHEMBL274993 2,6-DIBENZYLIDENECYCLOHEXANONE 1 9.59
CHEMBL482409 1 9.03
CHEMBL145927 4,4'-DIHYDROXYCHALCONE 1 9.02
CHEMBL129134 1 8.59
CHEMBL584437 1 7.87
CHEMBL138314 4,4'-DIMETHOXYCHALCONE 1 7.81
CHEMBL337821 1 6.85
CHEMBL140 CURCUMIN 3.0 1 6.70
CHEMBL128729 1 -
CHEMBL17205 CYCLOVALONE 2.0 1 -
CHEMBL482410 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17201 IC50 = 0.053 nM 10.28
CHEMBL276473 4'-HYDROXYCHALCONE IC50 = 0.12 nM 9.92
CHEMBL274993 2,6-DIBENZYLIDENECYCLOHEXANONE IC50 = 0.26 nM 9.59
CHEMBL482409 IC50 = 0.94 nM 9.03
CHEMBL145927 4,4'-DIHYDROXYCHALCONE IC50 = 0.96 nM 9.02
CHEMBL129134 IC50 = 2.58 nM 8.59
CHEMBL584437 IC50 = 13.37 nM 7.87
CHEMBL138314 4,4'-DIMETHOXYCHALCONE IC50 = 15.39 nM 7.81
CHEMBL337821 IC50 = 141.98 nM 6.85
CHEMBL140 CURCUMIN IC50 = 199.63 nM 6.70
CHEMBL128729 IC50 > 200.0 nM -
CHEMBL17205 CYCLOVALONE IC50 > 200.0 nM -
CHEMBL482410 IC50 > 200.0 nM -