Assay Detail
Binding
CHEMBL3631741
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Inhibition of thrombin-induced rabbit platelet aggregation after 4 hrs in presence of rabbit liver microsomes
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and antithrombotic evaluation of novel dabigatran etexilate analogs, a new series of non-peptides thrombin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.66 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539697 | DABIGATRAN ETEXILATE | 4.0 | 1 | 6.47 |
| CHEMBL3628001 | — | — | 1 | 6.22 |
| CHEMBL3629083 | — | — | 1 | 6.19 |
| CHEMBL3629086 | — | — | 1 | 6.14 |
| CHEMBL3629093 | — | — | 1 | 6.12 |
| CHEMBL3629089 | — | — | 1 | 6.08 |
| CHEMBL3629273 | — | — | 1 | 6.07 |
| CHEMBL3629087 | — | — | 1 | 6.06 |
| CHEMBL3629272 | — | — | 1 | 6.04 |
| CHEMBL3629269 | — | — | 1 | 5.92 |
| CHEMBL3629270 | — | — | 1 | 5.84 |
| CHEMBL3629094 | — | — | 1 | 5.82 |
| CHEMBL3629271 | — | — | 1 | 5.81 |
| CHEMBL3629088 | — | — | 1 | 5.48 |
| CHEMBL3629091 | — | — | 1 | 5.47 |
| CHEMBL3629084 | — | — | 1 | 5.39 |
| CHEMBL3629090 | — | — | 1 | 5.22 |
| CHEMBL3629267 | — | — | 1 | 5.06 |
| CHEMBL3629268 | — | — | 1 | 5.01 |
| CHEMBL3629266 | — | — | 1 | 4.86 |
| CHEMBL3629092 | — | — | 1 | 4.75 |
| CHEMBL3629085 | — | — | 1 | 4.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539697 | DABIGATRAN ETEXILATE | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3628001 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3629083 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3629086 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3629093 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3629089 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL3629273 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3629087 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3629272 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3629269 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL3629270 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL3629094 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL3629271 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL3629088 | — | IC50 | = | 3320.0 | nM | 5.48 |
| CHEMBL3629091 | — | IC50 | = | 3420.0 | nM | 5.47 |
| CHEMBL3629084 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL3629090 | — | IC50 | = | 5960.0 | nM | 5.22 |
| CHEMBL3629267 | — | IC50 | = | 8720.0 | nM | 5.06 |
| CHEMBL3629268 | — | IC50 | = | 9660.0 | nM | 5.01 |
| CHEMBL3629266 | — | IC50 | = | 13780.0 | nM | 4.86 |
| CHEMBL3629092 | — | IC50 | = | 17890.0 | nM | 4.75 |
| CHEMBL3629085 | — | IC50 | = | 27200.0 | nM | 4.57 |