| Index | Ligand Name | Structure | PDB code | Compound Potency nM |
| 1 | ui1 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1sqa | 0.62 |
| 2 | 497 | Substituted 2-Naphthamidine inhibitors of urokinase | 1owd | 6.3 |
| 3 | qgg | UROKINASE-TYPE PLASMINOGEN ACTIVATOR INHIBITOR COMPLEX WITH A 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE | 2vnt | 9.9 |
| 4 | 303 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1owk | 23.5 |
| 5 | 426 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1owi | 28 |
| 6 | ui2 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1sqo | 35 |
| 7 | 239 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1owh | 40 |
| 8 | d56 | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 2viw | 72 |
| 9 | 133 | ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS | 1gj8 | 110 |
| 10 | 655 | Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-Directed Serine Protease Inhibitors | 1o3p | 220 |
| 11 | vg2 | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 2viv | 520 |
| 12 | ui3 | Substituted 2-Naphthamidine Inhibitors of Urokinase | 1sqt | 630 |
| 13 | d55 | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 2viq | 1300 |
| 14 | 745 | Substituted 2-Naphthamadine inhibitors of Urokinase | 1u6q | 1310 |
| 15 | 135 | ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS | 1gja | 3800 |
| 16 | l1r | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 2vip | 5200 |
| 17 | amr | UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-AMILORIDE COMPLEX | 1f5l | 5300 |
| 18 | 123 | A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE | 1gi9 | 6000 |
| 19 | 136 | ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS | 1gjd | 6000 |
| 20 | cr9 | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | 1o5c | 6000 |
| 21 | que | Crystal structure of uPA in complex with quercetin | 5xg4 | 7000 |
| 22 | 4pg | Urokinase plasminogen activator B-chain-GPPE complex | 2r2w | 3.4e+004 |
| 23 | 11e | Synthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA | 4h42 | 3.41e+005 |