Assay Detail
Binding
CHEMBL5355126
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Inhibition of human factor Xa using S-2765 as chromogenic substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins
45
Total Activities
45
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 novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 5.23 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL198362 | RIVAROXABAN | 4.0 | 1 | 8.22 |
| CHEMBL5424963 | — | — | 1 | 7.00 |
| CHEMBL5409763 | — | — | 1 | 5.64 |
| CHEMBL5413299 | — | — | 1 | 5.62 |
| CHEMBL5427665 | — | — | 1 | 5.50 |
| CHEMBL5430493 | — | — | 1 | 5.37 |
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 5.24 |
| CHEMBL5425205 | — | — | 1 | 5.19 |
| CHEMBL5423783 | — | — | 1 | 5.17 |
| CHEMBL5429800 | — | — | 1 | 5.16 |
| CHEMBL1373768 | — | — | 1 | 5.10 |
| CHEMBL5418843 | — | — | 1 | 5.03 |
| CHEMBL5440166 | — | — | 1 | 5.00 |
| CHEMBL266349 | MELAGATRAN | 4.0 | 1 | 4.82 |
| CHEMBL5438252 | — | — | 1 | 4.65 |
| CHEMBL1560937 | — | — | 1 | 4.58 |
| CHEMBL5420305 | — | — | 1 | 4.55 |
| CHEMBL5424957 | — | — | 1 | 4.41 |
| CHEMBL5430930 | — | — | 1 | 4.17 |
| CHEMBL502016 | — | — | 1 | 4.15 |
| CHEMBL5425314 | — | — | 1 | - |
| CHEMBL5402933 | — | — | 1 | - |
| CHEMBL5397791 | — | — | 1 | - |
| CHEMBL5397540 | — | — | 1 | - |
| CHEMBL5432782 | — | — | 1 | - |
| CHEMBL5408843 | — | — | 1 | - |
| CHEMBL5426834 | — | — | 1 | - |
| CHEMBL5435750 | — | — | 1 | - |
| CHEMBL5429063 | — | — | 1 | - |
| CHEMBL5407846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL198362 | RIVAROXABAN | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5424963 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5409763 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5413299 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL5427665 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL5430493 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL48361 | DABIGATRAN | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL5425205 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5423783 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL5429800 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1373768 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5418843 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL5440166 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL266349 | MELAGATRAN | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL5438252 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL1560937 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5420305 | — | IC50 | = | 28300.0 | nM | 4.55 |
| CHEMBL5424957 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL5430930 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL502016 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL1444918 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1535020 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5418447 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5431421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5418604 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5420677 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5424153 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1575426 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5422724 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5395641 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5425457 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5409795 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5438043 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5427251 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5404225 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5407846 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5429063 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5435750 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426834 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5408843 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5432782 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5397540 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5397791 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5402933 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5425314 | — | IC50 | > | 100000.0 | nM | - |