Assay Detail
Binding
CHEMBL3871900
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Inhibition of human thrombin assessed as reduction in release of free nitroaniline using tosyl-glycyl-prolyl-arginine-4-nitranilide acetate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometer
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
Design, synthesis and antithrombotic evaluation of novel non-peptide thrombin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.58 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 8.22 |
| CHEMBL1166 | ARGATROBAN | 4.0 | 1 | 7.93 |
| CHEMBL3907547 | — | — | 1 | 7.08 |
| CHEMBL3969770 | — | — | 1 | 6.83 |
| CHEMBL3922260 | — | — | 1 | 6.36 |
| CHEMBL3950003 | — | — | 1 | 6.35 |
| CHEMBL3913261 | — | — | 1 | 6.34 |
| CHEMBL3958679 | — | — | 1 | 6.29 |
| CHEMBL3931186 | — | — | 1 | 6.00 |
| CHEMBL3977163 | — | — | 1 | 5.99 |
| CHEMBL3964811 | — | — | 1 | 5.84 |
| CHEMBL3978841 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48361 | DABIGATRAN | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1166 | ARGATROBAN | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3907547 | — | IC50 | = | 82.8 | nM | 7.08 |
| CHEMBL3969770 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL3922260 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL3950003 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL3913261 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL3958679 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL3931186 | — | IC50 | = | 1002.0 | nM | 6.00 |
| CHEMBL3977163 | — | IC50 | = | 1028.0 | nM | 5.99 |
| CHEMBL3964811 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL3978841 | — | IC50 | = | 1925.0 | nM | 5.72 |