Assay Detail
Binding
CHEMBL4357332
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Inhibition of human activated factor XI using pyro-Glu-Pro-Arg-pNA as substrate by spectrophotometry
17
Total Activities
17
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
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.34 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4089185 | — | — | 1 | 9.74 |
| CHEMBL4439729 | — | — | 1 | 9.74 |
| CHEMBL4444690 | — | — | 1 | 9.70 |
| CHEMBL4101766 | — | — | 1 | 9.41 |
| CHEMBL4456818 | — | — | 1 | 8.92 |
| CHEMBL4530525 | — | — | 1 | 8.68 |
| CHEMBL4534617 | — | — | 1 | 8.66 |
| CHEMBL4437236 | — | — | 1 | 8.47 |
| CHEMBL4438385 | — | — | 1 | 8.39 |
| CHEMBL4476061 | — | — | 1 | 8.26 |
| CHEMBL4470992 | — | — | 1 | 8.15 |
| CHEMBL4464434 | — | — | 1 | 7.96 |
| CHEMBL4552656 | — | — | 1 | 7.47 |
| CHEMBL4445384 | — | — | 1 | 7.42 |
| CHEMBL4585824 | — | — | 1 | 7.35 |
| CHEMBL4554665 | — | — | 1 | 6.78 |
| CHEMBL4563396 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4089185 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4439729 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4444690 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4101766 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL4456818 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4530525 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4534617 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4437236 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4438385 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL4476061 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4470992 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4464434 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4552656 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4445384 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4585824 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4554665 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL4563396 | — | Ki | = | 231.0 | nM | 6.64 |