Assay Detail
Binding
CHEMBL3854654
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Inhibition of full-length human TF/recombinant human factor 7a assessed as decrease in conversion of factor 10 to factor 10a by measuring S2765 hydrolysis after 15 mins
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Coagulation factor VII/tissue factor (CHEMBL2095194) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.84 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3891120 | — | — | 1 | 9.80 |
| CHEMBL3901391 | — | — | 1 | 9.64 |
| CHEMBL3978562 | — | — | 1 | 9.55 |
| CHEMBL3902498 | — | — | 1 | 9.37 |
| CHEMBL3917434 | — | — | 1 | 9.24 |
| CHEMBL3980787 | — | — | 1 | 9.21 |
| CHEMBL3909009 | — | — | 1 | 9.00 |
| CHEMBL3951940 | — | — | 1 | 8.66 |
| CHEMBL3930523 | — | — | 1 | 8.60 |
| CHEMBL3935309 | — | — | 1 | 8.26 |
| CHEMBL3942944 | — | — | 1 | 8.06 |
| CHEMBL3926417 | — | — | 1 | 7.82 |
| CHEMBL3907376 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3891120 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL3901391 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3978562 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3902498 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL3917434 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL3980787 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL3909009 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3951940 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3930523 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3935309 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3942944 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL3926417 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3907376 | — | Ki | = | 20.0 | nM | 7.70 |