An EC 3.4.24.* (metalloendopeptidase) inhibitor that interferes with the action of gelatinase A (EC 3.4.24.24).
ChEBI ID: 84036
| Member | Definition | Class |
|---|---|---|
| bis(pinacolato)diboron | A 1,3,2-dioxaborolane that is 4,4,5,5-tetramethyl-1,3,2-dioxaborolane in which the boron hydrogen at position 2 is replaced by a 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl group. It is a reagent used in organic synthesis to synthesise pinacol boronic esters. | bis(pinacolato)diboron |
| ilomastat | An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor | ilomastat |
| N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide | A hydroxamic acid that is N-hydroxy-D-valinamide in which the alpha-amino group has been substituted by isopropoxy and [biphenyl]-4-ylsulfonyl groups. A selective matrix metalloproteinase-2 (MMP-2) inhibitor, it is one of the most potent inducers of autophagy. Its physiological roles include angiogenesis, cancer metastasis, embryogenesis, tissue remodeling in development, and wound healing. | N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 6 (4.92) | 18.2507 |
| 2000's | 56 (45.90) | 29.6817 |
| 2010's | 46 (37.70) | 24.3611 |
| 2020's | 14 (11.48) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (0.81%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 122 (99.19%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Alpha-synuclein | Homo sapiens (human) | Potency | 16.3601 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 23.7101 | 2 | 2 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0810 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 2.2271 | 2 | 2 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 0.4731 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 5.8479 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 15.0816 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 21.4509 | 2 | 2 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 9.9303 | 2 | 2 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 7,307.8000 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 0.0675 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 11.2117 | 1 | 1 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 91.9997 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 37.6858 | 1 | 1 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 15.9848 | 2 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 28.3974 | 2 | 4 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 72 kDa type IV collagenase | Homo sapiens (human) | IC50 | 0.0026 | 16 | 16 |
| 72 kDa type IV collagenase | Homo sapiens (human) | Ki | 0.0004 | 3 | 3 |
| A disintegrin and metalloproteinase with thrombospondin motifs 4 | Homo sapiens (human) | IC50 | 0.4800 | 1 | 1 |
| A disintegrin and metalloproteinase with thrombospondin motifs 5 | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| Collagenase 3 | Homo sapiens (human) | IC50 | 0.0037 | 4 | 4 |
| Disintegrin and metalloproteinase domain-containing protein 10 | Homo sapiens (human) | IC50 | 0.1356 | 2 | 2 |
| Disintegrin and metalloproteinase domain-containing protein 12 | Homo sapiens (human) | IC50 | 0.0059 | 1 | 1 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | IC50 | 3.5844 | 4 | 4 |
| Disintegrin and metalloproteinase domain-containing protein 9 | Homo sapiens (human) | IC50 | 0.0286 | 2 | 2 |
| Elastase | Pseudomonas aeruginosa PAO1 | IC50 | 427.5000 | 2 | 2 |
| Interstitial collagenase | Homo sapiens (human) | IC50 | 0.0511 | 13 | 13 |
| Interstitial collagenase | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| Macrophage metalloelastase | Homo sapiens (human) | IC50 | 0.0050 | 8 | 8 |
| Matrilysin | Homo sapiens (human) | IC50 | 3.0373 | 3 | 4 |
| Matrix metalloproteinase-14 | Homo sapiens (human) | IC50 | 0.0102 | 12 | 12 |
| Matrix metalloproteinase-15 | Homo sapiens (human) | IC50 | 0.0060 | 2 | 2 |
| Matrix metalloproteinase-16 | Homo sapiens (human) | IC50 | 0.0223 | 3 | 3 |
| Matrix metalloproteinase-17 | Homo sapiens (human) | IC50 | 0.0034 | 1 | 1 |
| Matrix metalloproteinase-26 | Homo sapiens (human) | IC50 | 0.0170 | 2 | 2 |
| Matrix metalloproteinase-9 | Homo sapiens (human) | IC50 | 0.0041 | 15 | 15 |
| Matrix metalloproteinase-9 | Homo sapiens (human) | Ki | 0.0004 | 2 | 2 |
| Neutrophil collagenase | Homo sapiens (human) | IC50 | 0.0035 | 4 | 4 |
| Neutrophil collagenase | Homo sapiens (human) | Ki | 0.0002 | 2 | 2 |
| Prostaglandin G/H synthase 1 | Bos taurus (cattle) | IC50 | 0.0006 | 1 | 1 |
| Prostaglandin G/H synthase 2 | Bos taurus (cattle) | IC50 | 0.0006 | 1 | 1 |
| Stromelysin-1 | Homo sapiens (human) | IC50 | 0.0176 | 11 | 11 |
| Stromelysin-1 | Homo sapiens (human) | Ki | 0.0265 | 2 | 2 |
| Thermolysin | Bacillus thermoproteolyticus | IC50 | 608.0000 | 2 | 2 |