Assay Detail
Binding
CHEMBL902746
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Inhibition of human recombinant tPA
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 4.88 | 6.55 |
| Ki | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214814 | — | — | 1 | 6.55 |
| CHEMBL239118 | — | — | 1 | 5.43 |
| CHEMBL238708 | — | — | 1 | 5.40 |
| CHEMBL393979 | — | — | 1 | 5.21 |
| CHEMBL391968 | — | — | 1 | 5.16 |
| CHEMBL238491 | — | — | 1 | 5.14 |
| CHEMBL238493 | — | — | 1 | 5.10 |
| CHEMBL239535 | — | — | 1 | 4.92 |
| CHEMBL391916 | — | — | 1 | 4.80 |
| CHEMBL393591 | — | — | 1 | 4.64 |
| CHEMBL239747 | — | — | 1 | 4.44 |
| CHEMBL239331 | — | — | 1 | 4.36 |
| CHEMBL391344 | — | — | 1 | 4.36 |
| CHEMBL239536 | — | — | 1 | 4.24 |
| CHEMBL238707 | — | — | 1 | 4.18 |
| CHEMBL238913 | — | — | 1 | 4.17 |
| CHEMBL393592 | — | — | 1 | - |
| CHEMBL238902 | — | — | 1 | - |
| CHEMBL391969 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214814 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL239118 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL238708 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL393979 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL391968 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL238491 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL238493 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL239535 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL391916 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL393591 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL239747 | — | IC50 | = | 36600.0 | nM | 4.44 |
| CHEMBL239331 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL391344 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL239536 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL238707 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL238913 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL393592 | — | IC50 | = | 125000.0 | nM | - |
| CHEMBL238902 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL391969 | — | Ki | > | 1000000.0 | nM | - |