Assay Report Card

Basic Information

ID: ALA3705957

Type: Binding

Description: Enzyme Inhibition Assay: Enzyme activity is measured by observing the increase in fluorescence intensity caused by cleavage of a peptide substrate containing a fluorophore whose emission is quenched in the intact peptide.Assay buffer: 100 mM potassium phosphate pH 6.5, EDTA-Na 5 mM, Triton X-100 0.001%, DTT 5 mM.Enzymes (all at 1 nM): human and mouse Cathepsin S, Cat K, Cat B, Cat L.Substrate (20 μM): Z-Val-Val-Arg-AMC, except for Cat K which uses Z-Leu-Arg-AMC (both from Bachem).Z=Benzyloxycarbonyl.AMC=7-Amino-4-Methyl-Coumarin.DTT=dithiothreitol.Final volume: 100 μL.Excitation 360 nm, Emission 465 nm.Enzyme is added to the substance dilutions in 96-well microtitre plates and the reaction is started with substrate. Fluorescence emission is measured over 20 minutes, during which time a linear increase is observed in the absence of inhibitor.

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
678.603.503.50
578.481.851.85
592.512.202.20
746.594.434.43
791.044.544.54
646.482.792.79
690.932.902.90
710.513.763.76
754.963.873.87
666.563.633.63
711.013.743.74
566.441.981.98
610.892.092.09
624.922.442.44
638.952.832.83
708.923.033.03
664.472.932.93
684.554.124.12
729.004.234.23
778.615.315.31
823.065.425.42
584.432.472.47
628.882.582.58
823.065.075.07
722.943.423.42
678.493.663.66
722.943.773.77
736.973.773.77
757.675.355.35
802.125.465.46
657.563.703.70
702.013.813.81
746.654.384.38
791.104.494.49
646.532.732.73
690.982.842.84
786.984.404.40
750.953.293.29
780.983.903.90
804.974.704.70