Assay Detail
Binding
CHEMBL4003407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human thrombin preincubated for 10 mins followed by Ac-FVR-AMC substrate addition measured every 20s for 10 mins by fluorescence assay
12
Total Activities
12
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
Novel dabigatran derivatives with a fluorine atom at the C-2 position of the terminal benzene ring: Design, synthesis and anticoagulant activity evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.57 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4086267 | — | — | 1 | 9.08 |
| CHEMBL4094030 | — | — | 1 | 8.93 |
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 8.92 |
| CHEMBL4101764 | — | — | 1 | 8.85 |
| CHEMBL4095408 | — | — | 1 | 8.81 |
| CHEMBL4074973 | — | — | 1 | 8.65 |
| CHEMBL4102667 | — | — | 1 | 8.49 |
| CHEMBL3740791 | — | — | 1 | 8.48 |
| CHEMBL4076284 | — | — | 1 | 8.47 |
| CHEMBL4078405 | — | — | 1 | 8.43 |
| CHEMBL4087711 | — | — | 1 | 7.89 |
| CHEMBL4064792 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4086267 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL4094030 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL48361 | DABIGATRAN | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4101764 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL4095408 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL4074973 | — | IC50 | = | 2.26 | nM | 8.65 |
| CHEMBL4102667 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3740791 | — | IC50 | = | 3.33 | nM | 8.48 |
| CHEMBL4076284 | — | IC50 | = | 3.35 | nM | 8.47 |
| CHEMBL4078405 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4087711 | — | IC50 | = | 12.77 | nM | 7.89 |
| CHEMBL4064792 | — | IC50 | = | 14.6 | nM | 7.84 |