Assay Detail
Binding
CHEMBL3072496
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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 |
Publication
Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structureactivity relationships
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 | - |