Assay Detail
Binding
CHEMBL3636509
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Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin measured every 20 secs by spectrophotometric analysis
12
Total Activities
6
Compounds Tested
2
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 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.55 | 6.82 |
| pKinact | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3633251 | — | — | 2 | 6.82 |
| CHEMBL3633250 | — | — | 2 | 6.76 |
| CHEMBL3633460 | PF-06282999 | 1.0 | 2 | 6.50 |
| CHEMBL3633459 | — | — | 2 | 6.46 |
| CHEMBL3633248 | — | — | 2 | 6.43 |
| CHEMBL3633457 | — | — | 2 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3633251 | — | Ki | = | 151.36 | nM | 6.82 |
| CHEMBL3633250 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL3633460 | PF-06282999 | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL3633459 | — | Ki | = | 346.74 | nM | 6.46 |
| CHEMBL3633248 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL3633457 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL3633457 | — | pKinact | = | 2.43 | — | - |
| CHEMBL3633251 | — | pKinact | = | 2.34 | — | - |
| CHEMBL3633250 | — | pKinact | = | 2.61 | — | - |
| CHEMBL3633248 | — | pKinact | = | 2.41 | — | - |
| CHEMBL3633459 | — | pKinact | = | 2.38 | — | - |
| CHEMBL3633460 | PF-06282999 | pKinact | = | 2.43 | — | - |