Assay Detail
Binding
CHEMBL3419500
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human thrombin using Ac-FVR-AMC as substrate incubated for 10 mins prior to substrate addition measured for 10 min by fluorescence assay
23
Total Activities
23
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
Design, synthesis and structural exploration of novel fluorinated dabigatran derivatives as direct thrombin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.15 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 8.58 |
| CHEMBL3415214 | — | — | 1 | 8.49 |
| CHEMBL3415215 | — | — | 1 | 8.47 |
| CHEMBL3415062 | — | — | 1 | 8.46 |
| CHEMBL3415209 | — | — | 1 | 8.43 |
| CHEMBL3415059 | — | — | 1 | 8.34 |
| CHEMBL3415211 | — | — | 1 | 8.31 |
| CHEMBL3415058 | — | — | 1 | 8.31 |
| CHEMBL3415057 | — | — | 1 | 8.31 |
| CHEMBL3414580 | — | — | 1 | 8.31 |
| CHEMBL3415061 | — | — | 1 | 8.27 |
| CHEMBL3415064 | — | — | 1 | 8.25 |
| CHEMBL3415055 | — | — | 1 | 8.23 |
| CHEMBL3415056 | — | — | 1 | 8.21 |
| CHEMBL3415065 | — | — | 1 | 8.14 |
| CHEMBL3415210 | — | — | 1 | 8.08 |
| CHEMBL1166 | ARGATROBAN | 4.0 | 1 | 8.02 |
| CHEMBL3415213 | — | — | 1 | 7.87 |
| CHEMBL3415060 | — | — | 1 | 7.79 |
| CHEMBL3415216 | — | — | 1 | 7.72 |
| CHEMBL3415066 | — | — | 1 | 7.67 |
| CHEMBL3415212 | — | — | 1 | 7.63 |
| CHEMBL3415063 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48361 | DABIGATRAN | IC50 | = | 2.61 | nM | 8.58 |
| CHEMBL3415214 | — | IC50 | = | 3.23 | nM | 8.49 |
| CHEMBL3415215 | — | IC50 | = | 3.39 | nM | 8.47 |
| CHEMBL3415062 | — | IC50 | = | 3.49 | nM | 8.46 |
| CHEMBL3415209 | — | IC50 | = | 3.71 | nM | 8.43 |
| CHEMBL3415059 | — | IC50 | = | 4.54 | nM | 8.34 |
| CHEMBL3415211 | — | IC50 | = | 4.92 | nM | 8.31 |
| CHEMBL3415058 | — | IC50 | = | 4.84 | nM | 8.31 |
| CHEMBL3415057 | — | IC50 | = | 4.93 | nM | 8.31 |
| CHEMBL3414580 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3415061 | — | IC50 | = | 5.43 | nM | 8.27 |
| CHEMBL3415064 | — | IC50 | = | 5.63 | nM | 8.25 |
| CHEMBL3415055 | — | IC50 | = | 5.86 | nM | 8.23 |
| CHEMBL3415056 | — | IC50 | = | 6.13 | nM | 8.21 |
| CHEMBL3415065 | — | IC50 | = | 7.26 | nM | 8.14 |
| CHEMBL3415210 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1166 | ARGATROBAN | IC50 | = | 9.46 | nM | 8.02 |
| CHEMBL3415213 | — | IC50 | = | 13.61 | nM | 7.87 |
| CHEMBL3415060 | — | IC50 | = | 16.32 | nM | 7.79 |
| CHEMBL3415216 | — | IC50 | = | 19.16 | nM | 7.72 |
| CHEMBL3415066 | — | IC50 | = | 21.55 | nM | 7.67 |
| CHEMBL3415212 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL3415063 | — | IC50 | = | 23.96 | nM | 7.62 |