Assay Detail
Binding
CHEMBL5525869
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human Avi/10-his tagged GCase (40 to 536 residues) expressed baculovirus expression system in Sf9 cells in assessed as dissociation constant by isothermal titration calorimetry analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β-Glucocerebrosidase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 17 | 6.11 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5560927 | — | — | 1 | 7.75 |
| CHEMBL5567650 | — | — | 1 | 7.72 |
| CHEMBL5562071 | — | — | 1 | 7.30 |
| CHEMBL5562221 | — | — | 1 | 6.75 |
| CHEMBL5563159 | — | — | 1 | 6.66 |
| CHEMBL5567786 | — | — | 1 | 6.60 |
| CHEMBL5565566 | — | — | 1 | 6.52 |
| CHEMBL5560175 | — | — | 1 | 6.51 |
| CHEMBL5563549 | — | — | 1 | 6.00 |
| CHEMBL5555937 | — | — | 1 | 5.96 |
| CHEMBL5559958 | — | — | 1 | 5.52 |
| CHEMBL5560911 | — | — | 1 | 5.16 |
| CHEMBL144129 | — | — | 1 | 4.72 |
| CHEMBL558 | MEXILETINE | 4.0 | 1 | 4.43 |
| CHEMBL5555347 | — | — | 1 | 4.00 |
| CHEMBL5564772 | — | — | 1 | - |
| CHEMBL5561451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5560927 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL5567650 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL5562071 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL5562221 | — | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL5563159 | — | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL5567786 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL5565566 | — | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL5560175 | — | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL5563549 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL5555937 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL5559958 | — | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL5560911 | — | Kd | = | 7000.0 | nM | 5.16 |
| CHEMBL144129 | — | Kd | = | 19000.0 | nM | 4.72 |
| CHEMBL558 | MEXILETINE | Kd | = | 37000.0 | nM | 4.43 |
| CHEMBL5555347 | — | Kd | = | 100000.0 | nM | 4.00 |
| CHEMBL5564772 | — | Kd | = | 180000.0 | nM | - |
| CHEMBL5561451 | — | Kd | = | 410000.0 | nM | - |