Assay Detail
Binding
CHEMBL5730286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: Plasma kallikrein determinations were made in 0.1 M sodium phosphate buffer at a pH of 7.5 containing 0.1-0.2 M sodium chloride and 0.5% PEG 8000. Determinations were made using purified human plasma kallikrein (Enzyme Research Laboratories) at a final assay concentration of 200 pM and the synthetic substrate S-2302 (H-(D)-Pro-Phe-Arg-pNA; CHROMOGENIX®) at a concentration of 0.00008-0.0004 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 | 7.62 | 8.00 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4108841 | — | — | 3 | 8.00 |
| CHEMBL4113006 | — | — | 6 | 7.77 |
| CHEMBL4111839 | — | — | 6 | 7.66 |
| CHEMBL4107758 | — | — | 6 | 7.62 |
| CHEMBL4112929 | MILVEXIAN | 3.0 | 3 | 7.55 |
| CHEMBL4115014 | — | — | 3 | 7.48 |
| CHEMBL4107075 | — | — | 3 | 7.46 |
| CHEMBL4107761 | — | — | 3 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4108841 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4113006 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4113006 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4111839 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4111839 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4107758 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4112929 | MILVEXIAN | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4107758 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4115014 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4107075 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4107761 | — | Ki | = | 37.0 | nM | 7.43 |
| 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 | - |