Assay Detail
Binding
CHEMBL927669
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Inhibition of uPA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Urokinase-type plasminogen activator (CHEMBL3286) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.96 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL252937 | — | — | 1 | 7.70 |
| CHEMBL111576 | — | — | 1 | 7.43 |
| CHEMBL253825 | — | — | 1 | 7.14 |
| CHEMBL107955 | — | — | 1 | 6.39 |
| CHEMBL252166 | — | — | 1 | 6.34 |
| CHEMBL253608 | — | — | 1 | 6.28 |
| CHEMBL253607 | — | — | 1 | 6.14 |
| CHEMBL401365 | — | — | 1 | 5.89 |
| CHEMBL401366 | — | — | 1 | 5.80 |
| CHEMBL253379 | — | — | 1 | 5.57 |
| CHEMBL398428 | — | — | 1 | 5.28 |
| CHEMBL253378 | — | — | 1 | 4.64 |
| CHEMBL253377 | — | — | 1 | 4.46 |
| CHEMBL401484 | — | — | 1 | 4.40 |
| CHEMBL147507 | (R)-MEXILETINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL252937 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL111576 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL253825 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL107955 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL252166 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL253608 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL253607 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL401365 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL401366 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL253379 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL398428 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL253378 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL253377 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL401484 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL147507 | (R)-MEXILETINE | IC50 | > | 1000000.0 | nM | - |