Assay Detail
Binding
CHEMBL3854659
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Inhibition of human HK1 using H-D-Val-Leu-Arg-AFC as substrate assessed as release of AFC after 10 to 120 mins by spectrofluorimetric method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.53 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907376 | — | — | 1 | 7.68 |
| CHEMBL3935309 | — | — | 1 | 7.47 |
| CHEMBL3909009 | — | — | 1 | 7.00 |
| CHEMBL3951940 | — | — | 1 | 6.70 |
| CHEMBL3942944 | — | — | 1 | 6.58 |
| CHEMBL3891120 | — | — | 1 | 6.57 |
| CHEMBL3980787 | — | — | 1 | 6.41 |
| CHEMBL3926417 | — | — | 1 | 6.24 |
| CHEMBL3917434 | — | — | 1 | 6.22 |
| CHEMBL3902498 | — | — | 1 | 6.19 |
| CHEMBL3930523 | — | — | 1 | 6.19 |
| CHEMBL3901391 | — | — | 1 | 6.10 |
| CHEMBL3978562 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907376 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3935309 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3909009 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3951940 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3942944 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3891120 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL3980787 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL3926417 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL3917434 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3902498 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL3930523 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL3901391 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL3978562 | — | Ki | = | 2600.0 | nM | 5.58 |