Assay Detail
Binding
CHEMBL3743968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human uPA using pyro-Glu-Gly-Arg-pNA as substrate assessed as para-nitroaniline release from substrate measured for 5 mins by spectrophotometric assay
39
Total Activities
39
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 |
Target
Urokinase-type plasminogen activator (CHEMBL3286) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.09 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3740183 | — | — | 1 | 7.01 |
| CHEMBL3740973 | — | — | 1 | 6.76 |
| CHEMBL3741622 | — | — | 1 | 6.74 |
| CHEMBL3741173 | — | — | 1 | 6.59 |
| CHEMBL3740904 | — | — | 1 | 6.44 |
| CHEMBL3741100 | — | — | 1 | 6.39 |
| CHEMBL87563 | GABEXATE | 3.0 | 1 | 6.37 |
| CHEMBL3742152 | — | — | 1 | 5.16 |
| CHEMBL1945236 | — | — | 1 | 5.06 |
| CHEMBL3740931 | — | — | 1 | 5.04 |
| CHEMBL3740914 | — | — | 1 | 5.03 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 4.92 |
| CHEMBL3740642 | — | — | 1 | 4.83 |
| CHEMBL3740676 | — | — | 1 | 4.74 |
| CHEMBL3739833 | — | — | 1 | 4.71 |
| CHEMBL3741004 | — | — | 1 | 4.62 |
| CHEMBL3739519 | — | — | 1 | 4.57 |
| CHEMBL3740294 | — | — | 1 | 4.56 |
| CHEMBL3741887 | — | — | 1 | 4.56 |
| CHEMBL3740145 | — | — | 1 | 4.52 |
| CHEMBL3741697 | — | — | 1 | 4.52 |
| CHEMBL3742000 | — | — | 1 | 4.32 |
| CHEMBL3740795 | — | — | 1 | 4.27 |
| CHEMBL3740195 | — | — | 1 | 4.24 |
| CHEMBL3741341 | — | — | 1 | 4.22 |
| CHEMBL3739939 | — | — | 1 | 4.19 |
| CHEMBL3741486 | — | — | 1 | 4.00 |
| CHEMBL3740693 | — | — | 1 | 4.00 |
| CHEMBL3741860 | — | — | 1 | - |
| CHEMBL3740528 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3740183 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3740973 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3741622 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3741173 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL3740904 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL3741100 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL87563 | GABEXATE | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL3742152 | — | IC50 | = | 6890.0 | nM | 5.16 |
| CHEMBL1945236 | — | IC50 | = | 8670.0 | nM | 5.06 |
| CHEMBL3740931 | — | IC50 | = | 9040.0 | nM | 5.04 |
| CHEMBL3740914 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL945 | AMILORIDE | IC50 | = | 11980.0 | nM | 4.92 |
| CHEMBL3740642 | — | IC50 | = | 14950.0 | nM | 4.83 |
| CHEMBL3740676 | — | IC50 | = | 18030.0 | nM | 4.74 |
| CHEMBL3739833 | — | IC50 | = | 19390.0 | nM | 4.71 |
| CHEMBL3741004 | — | IC50 | = | 23890.0 | nM | 4.62 |
| CHEMBL3739519 | — | IC50 | = | 26850.0 | nM | 4.57 |
| CHEMBL3740294 | — | IC50 | = | 27440.0 | nM | 4.56 |
| CHEMBL3741887 | — | IC50 | = | 27260.0 | nM | 4.56 |
| CHEMBL3740145 | — | IC50 | = | 30150.0 | nM | 4.52 |
| CHEMBL3741697 | — | IC50 | = | 30250.0 | nM | 4.52 |
| CHEMBL3742000 | — | IC50 | = | 48470.0 | nM | 4.32 |
| CHEMBL3740795 | — | IC50 | = | 53780.0 | nM | 4.27 |
| CHEMBL3740195 | — | IC50 | = | 57550.0 | nM | 4.24 |
| CHEMBL3741341 | — | IC50 | = | 60840.0 | nM | 4.22 |
| CHEMBL3739939 | — | IC50 | = | 63920.0 | nM | 4.19 |
| CHEMBL3741486 | — | IC50 | = | 99160.0 | nM | 4.00 |
| CHEMBL3740693 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3739955 | — | IC50 | = | 200000.0 | nM | - |
| CHEMBL3740173 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL3739666 | — | IC50 | = | 125000.0 | nM | - |
| CHEMBL3741372 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL3741137 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL3740839 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3740414 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL3741382 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3740983 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3740528 | — | IC50 | = | 200000.0 | nM | - |
| CHEMBL3741860 | — | IC50 | > | 1000000.0 | nM | - |