| DB02118 | CP-271485 | experimental | unknown | | Details |
| DB00551 | Acetohydroxamic acid | approved | unknown | inhibitor | Details |
| DB03367 | PF-00356231 | experimental | unknown | | Details |
| DB03880 | Batimastat | experimental | unknown | | Details |
| DB04405 | 2-[2-(1,3-Dioxo-1,3-Dihydro-2h-Isoindol-2-Yl)Ethyl]-4-(4'-Ethoxy-1,1'-Biphenyl-4-Yl)-4-Oxobutanoic Acid | experimental | unknown | | Details |
| DB05387 | Neovastat | investigational | unknown | | Details |
| DB00786 | Marimastat | investigational | yes | inhibitor | Details |
| DB07026 | (1S,5S,7R)-N~7~-(BIPHENYL-4-YLMETHYL)-N~3~-HYDROXY-6,8-DIOXA-3-AZABICYCLO[3.2.1]OCTANE-3,7-DICARBOXAMIDE | experimental | unknown | | Details |
| DB07446 | N-(biphenyl-4-ylsulfonyl)-D-leucine | experimental | unknown | | Details |
| DB07556 | CGS-27023 | experimental | unknown | | Details |
| DB07683 | N-(dibenzo[b,d]thiophen-3-ylsulfonyl)-L-valine | experimental | unknown | | Details |
| DB07920 | N-oxo-2-[(4-phenylphenyl)sulfonylamino]ethanamide | experimental | unknown | | Details |
| DB07921 | 2-[(4-fluorophenyl)sulfonylamino]-N-oxo-ethanamide | experimental | unknown | | Details |
| DB07922 | N-oxo-2-(phenylsulfonylamino)ethanamide | experimental | unknown | | Details |
| DB08271 | N-ISOBUTYL-N-[4-METHOXYPHENYLSULFONYL]GLYCYL HYDROXAMIC ACID | experimental | unknown | | Details |
| DB08599 | N-[(4-methoxyphenyl)sulfonyl]-D-alanine | experimental | unknown | | Details |
| DB00013 | Urokinase | approved, investigational, withdrawn | unknown | substrate | Details |