Basic Information
ID: ALA3888092
Type: Binding
Description: Cathepsin 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%, DDT 5 mM. Enzymes (all at 1 nM): human and mouse Cathepsin S, Cat K, Cat B, Cat LSubstrate (20 uM): 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. Final volume: 100 uL. 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
Bioactivity
Activity Types for Assay ALA3888092
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 500.02 | 4.13 | 4.13 |
| 483.95 | 3.41 | 3.41 |
| 488.37 | 4.06 | 4.06 |
| 471.92 | 3.54 | 3.54 |
| 487.89 | 3.46 | 3.46 |
| 545.38 | 3.36 | 3.36 |
| 532.82 | 4.17 | 4.17 |
| 521.92 | 4.42 | 4.42 |
| 478.94 | 3.28 | 3.28 |
| 509.01 | 3.09 | 3.09 |
| 521.92 | 4.42 | 4.42 |
| 579.82 | 4.01 | 4.01 |
| 453.93 | 3.40 | 3.40 |
| 481.98 | 3.97 | 3.97 |
| 489.91 | 3.68 | 3.68 |
| 609.12 | 4.74 | 4.74 |
| 488.37 | 4.06 | 4.06 |
| 508.02 | 4.28 | 4.28 |
| 519.91 | 4.20 | 4.20 |
| 543.36 | 3.13 | 3.13 |
| 487.89 | 3.46 | 3.46 |
| 498.00 | 3.90 | 3.90 |
| 460.94 | 2.29 | 2.29 |
| 479.96 | 3.74 | 3.74 |
| 506.99 | 2.87 | 2.87 |
| 415.49 | 3.08 | 3.08 |
| 476.92 | 3.05 | 3.05 |
| 486.36 | 3.83 | 3.83 |
| 607.11 | 4.52 | 4.52 |
| 481.94 | 3.19 | 3.19 |
| 530.81 | 3.94 | 3.94 |
| 519.91 | 4.20 | 4.20 |
| 482.99 | 3.60 | 3.60 |
| 417.47 | 2.53 | 2.53 |
| 529.82 | 3.98 | 3.98 |
| 577.81 | 3.79 | 3.79 |
| 504.35 | 3.97 | 3.97 |
| 451.91 | 3.18 | 3.18 |
| 442.95 | 2.34 | 2.34 |
| 451.91 | 3.18 | 3.18 |
| 487.89 | 3.46 | 3.46 |
| 486.36 | 3.83 | 3.83 |
| 417.47 | 2.53 | 2.53 |
| 471.00 | 2.98 | 2.98 |
| 478.93 | 2.59 | 2.59 |
| 449.94 | 3.73 | 3.73 |
| 450.93 | 3.21 | 3.21 |
| 469.90 | 3.32 | 3.32 |
| 506.00 | 4.06 | 4.06 |