Assay Detail
Binding
CHEMBL5737263
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Factor XIa assay : Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 145 mM NaCl, 5 mM KCl, and 0.1% PEG 8000 (polyethylene glycol; JT Baker or Fisher Scientific). Determinations were made using purified human Factor XIa at a final concentration of 25-200 pM (Haematologic Technologies) and the synthetic substrate S-2366 (pyroGlu-Pro-Arg-pNA; CHROMOGENIX® or AnaSpec) at a concentration of 0.0002-0.001 M.
33
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrimidinones as factor XIA inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.82 | 10.00 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4112929 | MILVEXIAN | 3.0 | 3 | 10.00 |
| CHEMBL4107758 | — | — | 6 | 10.00 |
| CHEMBL4115014 | — | — | 3 | 10.00 |
| CHEMBL4113006 | — | — | 6 | 10.00 |
| CHEMBL4111839 | — | — | 6 | 9.70 |
| CHEMBL4107075 | — | — | 3 | 9.70 |
| CHEMBL4107761 | — | — | 3 | 9.70 |
| CHEMBL4108841 | — | — | 3 | 9.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4115014 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4113006 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4113006 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4107758 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4112929 | MILVEXIAN | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4107758 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4107761 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4111839 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4107075 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4111839 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4108841 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4107758 | — | k_off | = | - | s-1 | - |
| CHEMBL4107758 | — | k_off | = | - | s-1 | - |
| CHEMBL4107758 | — | kon | = | - | — | - |
| CHEMBL4111839 | — | k_off | = | - | s-1 | - |
| CHEMBL4111839 | — | kon | = | - | — | - |
| CHEMBL4111839 | — | k_off | = | - | s-1 | - |
| CHEMBL4111839 | — | kon | = | - | — | - |
| CHEMBL4108841 | — | k_off | = | - | s-1 | - |
| CHEMBL4108841 | — | kon | = | - | — | - |
| CHEMBL4112929 | MILVEXIAN | k_off | = | - | s-1 | - |
| CHEMBL4112929 | MILVEXIAN | kon | = | - | — | - |
| CHEMBL4115014 | — | kon | = | - | — | - |
| CHEMBL4115014 | — | k_off | = | - | s-1 | - |
| CHEMBL4107761 | — | k_off | = | - | s-1 | - |
| CHEMBL4107761 | — | kon | = | - | — | - |
| CHEMBL4107075 | — | k_off | = | - | s-1 | - |
| CHEMBL4107075 | — | kon | = | - | — | - |
| CHEMBL4107758 | — | kon | = | - | — | - |
| CHEMBL4113006 | — | kon | = | - | — | - |
| CHEMBL4113006 | — | k_off | = | - | s-1 | - |
| CHEMBL4113006 | — | kon | = | - | — | - |
| CHEMBL4113006 | — | k_off | = | - | s-1 | - |