Assay Detail
Binding
CHEMBL4407126
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Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
22
Total Activities
22
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
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.36 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3728620 | — | — | 1 | 8.10 |
| CHEMBL3728724 | — | — | 1 | 7.13 |
| CHEMBL3728462 | — | — | 1 | 6.92 |
| CHEMBL3732386 | — | — | 1 | 6.62 |
| CHEMBL3931873 | — | — | 1 | 6.62 |
| CHEMBL3728507 | — | — | 1 | 6.57 |
| CHEMBL4439280 | — | — | 1 | 6.46 |
| CHEMBL3732490 | — | — | 1 | 6.00 |
| CHEMBL3731720 | — | — | 1 | 5.75 |
| CHEMBL3727598 | — | — | 1 | 5.68 |
| CHEMBL3732510 | — | — | 1 | 5.68 |
| CHEMBL3729282 | — | — | 1 | 5.62 |
| CHEMBL3730957 | — | — | 1 | 5.51 |
| CHEMBL3728010 | — | — | 1 | - |
| CHEMBL4471641 | — | — | 1 | - |
| CHEMBL4444227 | — | — | 1 | - |
| CHEMBL4435447 | — | — | 1 | - |
| CHEMBL4572935 | — | — | 1 | - |
| CHEMBL3730643 | — | — | 1 | - |
| CHEMBL3728130 | — | — | 1 | - |
| CHEMBL3731871 | — | — | 1 | - |
| CHEMBL3732594 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3728620 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3728724 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3728462 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3732386 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3931873 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3728507 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4439280 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3732490 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3731720 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3727598 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3732510 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3729282 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3730957 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3728010 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4471641 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4444227 | — | IC50 | - | — | - | |
| CHEMBL4435447 | — | IC50 | - | — | - | |
| CHEMBL4572935 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3730643 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3728130 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3731871 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3732594 | — | IC50 | > | 30000.0 | nM | - |