Assay Detail
Binding
CHEMBL4676505
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human coagulation factor XIIA using Boc-Gln-Gly-Arg-AMC as fluorogenic substrate measured at 1 min interval for 1 hr by fluorometric assay
37
Total Activities
37
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
Acylated 1H-1,2,4-Triazol-5-amines Targeting Human Coagulation Factor XIIa and Thrombin: Conventional and Microscale Synthesis, Anticoagulant Properties, and Mechanism of Action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.35 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4776259 | — | — | 1 | 7.54 |
| CHEMBL4786270 | — | — | 1 | 7.21 |
| CHEMBL4777212 | — | — | 1 | 7.04 |
| CHEMBL4783236 | — | — | 1 | 7.03 |
| CHEMBL4746556 | — | — | 1 | 6.97 |
| CHEMBL4761275 | — | — | 1 | 6.96 |
| CHEMBL4748137 | — | — | 1 | 6.88 |
| CHEMBL4760132 | — | — | 1 | 6.87 |
| CHEMBL4754247 | — | — | 1 | 6.86 |
| CHEMBL4749147 | — | — | 1 | 6.85 |
| CHEMBL4750895 | — | — | 1 | 6.79 |
| CHEMBL4740475 | — | — | 1 | 6.68 |
| CHEMBL4786773 | — | — | 1 | 6.54 |
| CHEMBL4797183 | — | — | 1 | 6.53 |
| CHEMBL4754712 | — | — | 1 | 6.51 |
| CHEMBL2151128 | — | — | 1 | 6.27 |
| CHEMBL4780154 | — | — | 1 | 6.21 |
| CHEMBL4781896 | — | — | 1 | 6.10 |
| CHEMBL4764774 | — | — | 1 | 6.01 |
| CHEMBL4762106 | — | — | 1 | 5.81 |
| CHEMBL4749335 | — | — | 1 | 5.79 |
| CHEMBL4759962 | — | — | 1 | 5.49 |
| CHEMBL4800151 | — | — | 1 | 5.23 |
| CHEMBL4800646 | — | — | 1 | 5.01 |
| CHEMBL4764057 | — | — | 1 | 4.92 |
| CHEMBL4744082 | — | — | 1 | 4.88 |
| CHEMBL1568624 | — | — | 1 | - |
| CHEMBL295684 | — | — | 1 | - |
| CHEMBL432863 | — | — | 1 | - |
| CHEMBL4791078 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4776259 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4786270 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4777212 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4783236 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4746556 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4761275 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4748137 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4760132 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4754247 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4749147 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4750895 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4740475 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4786773 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4797183 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL4754712 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL2151128 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL4780154 | — | IC50 | = | 617.0 | nM | 6.21 |
| CHEMBL4781896 | — | IC50 | = | 793.0 | nM | 6.10 |
| CHEMBL4764774 | — | IC50 | = | 968.0 | nM | 6.01 |
| CHEMBL4762106 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL4749335 | — | IC50 | = | 1606.0 | nM | 5.79 |
| CHEMBL4759962 | — | IC50 | = | 3207.0 | nM | 5.49 |
| CHEMBL4800151 | — | IC50 | = | 5934.0 | nM | 5.23 |
| CHEMBL4800646 | — | IC50 | = | 9822.0 | nM | 5.01 |
| CHEMBL4764057 | — | IC50 | = | 12130.0 | nM | 4.92 |
| CHEMBL4744082 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL4761623 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL198362 | RIVAROXABAN | IC50 | > | 33000.0 | nM | - |
| CHEMBL48361 | DABIGATRAN | IC50 | > | 33000.0 | nM | - |
| CHEMBL4753362 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4755409 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4748586 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4756713 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4791078 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL432863 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL295684 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1568624 | — | IC50 | > | 5000.0 | nM | - |