Assay Detail
Binding
CHEMBL3705635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Inhibition Assay: The enzyme inhibition assays used monitored the ability of a test compound to bind and prevent the hydrolysis of a fluorogenic substrate in a concentration-dependent mariner. Specifically, the enzyme activity of recombinant human GCase (rhGCase; Cerezyme, Genzyme Corp.) was measured using the 4-methylumbelliferyl-β-D-glucopyranoside (4-MU-β-D-Glc) fluorogenic substrate in the absence or in the presence of varying amounts of each test compound.
36
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Compositions for preventing and/or treating degenerative disorders of the central nervous system
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.53 | 9.05 |
| IC50 | 18 | 7.15 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3684925 | — | — | 8 | 9.05 |
| CHEMBL3684924 | — | — | 4 | 8.51 |
| CHEMBL3684928 | — | — | 4 | 8.05 |
| CHEMBL3684926 | — | — | 8 | 8.00 |
| CHEMBL3684929 | — | — | 4 | 7.82 |
| CHEMBL3684930 | — | — | 4 | 7.51 |
| CHEMBL3684927 | — | — | 4 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3684925 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3684924 | — | Ki | = | 3.06 | nM | 8.51 |
| CHEMBL3684925 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3684924 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3684925 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3684928 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL3684926 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3684924 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL3684929 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3684925 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3684928 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3684925 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3684926 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3684924 | — | IC50 | = | 25.9 | nM | 7.59 |
| CHEMBL3684929 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3684930 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL3684926 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3684925 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3684926 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3684925 | — | Ki | = | 49.8 | nM | 7.30 |
| CHEMBL3684930 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3684926 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3684927 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL3684925 | — | IC50 | = | 94.6 | nM | 7.02 |
| CHEMBL3684929 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL3684926 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3684930 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL3684927 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3684926 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL3684929 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL3684927 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL3684930 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL3684926 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL3684927 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL3684928 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL3684928 | — | IC50 | = | 3290.0 | nM | 5.48 |