| Solution Information | help | |
| Enzyme: | Procathepsin L | |
| inhibitor: | BDBM49365 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this counterscreen assay is to determine dose response curves for compounds identified as active in a set of previous experiments entitled, "QFRET-based biochemical high throughput confirmation assay for inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PFM18AAP)" (AID 2178). In this biochemical assay, a commercially available fluorogenic peptide substrate (Z-Leu-Arg-MCA) is incubated with purified recombinant cathepsin L1 protein in the presence of test compounds. Cleavage of the substrate by cathepsin L1 releases the fluorogenic MCA leaving group, leading to an increase in well fluorescence. As designed, compounds that inhibit cathepsin L1 will prevent substrate cleavage and liberation of the fluorescent leaving group, resulting in decreased well fluorescence. Test compounds were assayed in triplicate in a 10-point 1:3 dilution series starting at a nominal test concentration of 59.6 micromolar. Protocol Summary: Prior to the start | |
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