Assay Detail
Binding
CHEMBL5732496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Activity Assay: Human Factor XIa (Haematologic Technologies Inc.) activity was measured at an enzyme concentration of 0.1 U/mL in 150 mM NaCl, 5 mM KCl, 1 mg/mL PEG6000, 50 mM HEPES-NaOH (pH7.4) with 300 μM S-2366 (pyroGlu-Pro-Arg-pNA, Chromogenix).
108
Total Activities
33
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
Pyridinone and pyrimidinone derivatives as factor Xia
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.27 | 8.96 |
| kon | 36 | - | - |
| k_off | 36 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6004391 | — | — | 3 | 8.96 |
| CHEMBL5846555 | — | — | 3 | 8.96 |
| CHEMBL5766585 | — | — | 3 | 8.85 |
| CHEMBL6032526 | — | — | 3 | 8.82 |
| CHEMBL5945565 | — | — | 3 | 8.80 |
| CHEMBL5884875 | — | — | 3 | 8.80 |
| CHEMBL5882548 | — | — | 3 | 8.77 |
| CHEMBL6026982 | — | — | 3 | 8.68 |
| CHEMBL5397198 | — | — | 6 | 8.62 |
| CHEMBL5978713 | — | — | 3 | 8.60 |
| CHEMBL5967704 | — | — | 3 | 8.55 |
| CHEMBL3398640 | — | — | 3 | 8.44 |
| CHEMBL5939704 | — | — | 3 | 8.42 |
| CHEMBL6059084 | — | — | 3 | 8.41 |
| CHEMBL6054374 | — | — | 3 | 8.38 |
| CHEMBL6057699 | — | — | 3 | 8.34 |
| CHEMBL5865530 | — | — | 3 | 8.32 |
| CHEMBL5989668 | — | — | 3 | 8.31 |
| CHEMBL6051428 | — | — | 3 | 8.24 |
| CHEMBL5833820 | — | — | 3 | 8.21 |
| CHEMBL5905676 | — | — | 6 | 8.19 |
| CHEMBL5776257 | — | — | 3 | 8.14 |
| CHEMBL5753217 | — | — | 3 | 8.08 |
| CHEMBL5773636 | — | — | 3 | 7.96 |
| CHEMBL5945125 | — | — | 3 | 7.96 |
| CHEMBL6039339 | — | — | 3 | 7.89 |
| CHEMBL5986345 | — | — | 3 | 7.85 |
| CHEMBL5429306 | — | — | 6 | 7.82 |
| CHEMBL6041447 | — | — | 3 | 7.77 |
| CHEMBL5784275 | — | — | 3 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5846555 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6004391 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5766585 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL6032526 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5884875 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5945565 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5882548 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL6026982 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5397198 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5397198 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5978713 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5967704 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3398640 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5939704 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL6059084 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL6054374 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL6057699 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5865530 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5989668 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL6051428 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5833820 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5905676 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5905676 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5776257 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5753217 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5945125 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5773636 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6039339 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5986345 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5429306 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5429306 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6041447 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5784275 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5758488 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5964592 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5397198 | — | k_off | = | - | s-1 | - |
| CHEMBL5784275 | — | k_off | = | - | s-1 | - |
| CHEMBL3398640 | — | k_off | = | - | s-1 | - |
| CHEMBL5784275 | — | kon | = | - | — | - |
| CHEMBL3398640 | — | kon | = | - | — | - |
| CHEMBL5846555 | — | k_off | = | - | s-1 | - |
| CHEMBL5846555 | — | kon | = | - | — | - |
| CHEMBL6026982 | — | k_off | = | - | s-1 | - |
| CHEMBL6026982 | — | kon | = | - | — | - |
| CHEMBL6004391 | — | k_off | = | - | s-1 | - |
| CHEMBL6004391 | — | kon | = | - | — | - |
| CHEMBL5884875 | — | k_off | = | - | s-1 | - |
| CHEMBL5884875 | — | kon | = | - | — | - |
| CHEMBL5787109 | — | k_off | = | - | s-1 | - |
| CHEMBL5766585 | — | k_off | = | - | s-1 | - |