Assay Detail
Binding
CHEMBL4035783
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cytosolic endo-beta-N-acetylglucosaminidase (CHEMBL5172) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Repurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.77 | 5.35 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1219 | RABEPRAZOLE | 4.0 | 1 | 5.35 |
| CHEMBL1475252 | TENATOPRAZOLE | 2.0 | 1 | 4.70 |
| CHEMBL480 | LANSOPRAZOLE | 4.0 | 1 | 4.61 |
| CHEMBL1201863 | DEXLANSOPRAZOLE | 4.0 | 1 | 4.60 |
| CHEMBL1503 | OMEPRAZOLE | 4.0 | 1 | 4.60 |
| CHEMBL1200470 | ESOMEPRAZOLE SODIUM | 4.0 | 1 | - |
| CHEMBL3989559 | PANTOPRAZOLE SODIUM | 4.0 | 1 | - |
| CHEMBL4076068 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1219 | RABEPRAZOLE | IC50 | = | 4470.0 | nM | 5.35 |
| CHEMBL1475252 | TENATOPRAZOLE | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL480 | LANSOPRAZOLE | IC50 | = | 24380.0 | nM | 4.61 |
| CHEMBL1201863 | DEXLANSOPRAZOLE | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1503 | OMEPRAZOLE | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1200470 | ESOMEPRAZOLE SODIUM | Inhibition | - | % | - | |
| CHEMBL3989559 | PANTOPRAZOLE SODIUM | Inhibition | - | % | - | |
| CHEMBL4076068 | — | Inhibition | - | % | - |