蛋白酶抑制剂
Proteases are enzymes that catalyze proteolysis and can be found in all forms of life, even in viruses. The proteolysis process is realized by cleaving peptide bonds within proteins. Proteases control a variety of physiological processes such as immune response, cell cycle, cell death, wound healing, and food digestion. This fact makes proteases an important group of molecular targets for metabolic disease treatment, as well as the treatment of pathogenic diseases caused by bacteria or viruses.
Protease Inhibitors Library is composed of 777 small ligands. The collection includes compounds with activity against metabolic diseases; inhibitors of ACE2 metalloprotease, which is responsible for SARS-CoV-2 cell entry; ligands with broad-scope antiviral activity; antiprotozoal compounds.
Related terms: methionyl aminopeptidase, dipeptidyl peptidase, cathepsin B, monoacylglycerol lipase, MMP2, MMP8, serine protease, MMP13, angiotensin-converting enzyme
Structure of metalloprotease ACE2, PDBID = 1R42
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Highlights
Saxagliptin, an anti-diabet type 2
MLN-4760 ACE2 inhibitor
Tenofovir, antiviral
Atovaquone, antiprotozoal
Product Features
A set of 777 NHR-binding molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target broad scope of human and pathogenic proteases.
Protease Inhibitors Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.87.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficient values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
