Assay Detail
Binding
CHEMBL3749465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transitional endoplasmic reticulum ATPase (CHEMBL1075145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.60 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3747448 | — | — | 1 | 6.30 |
| CHEMBL3747513 | CB-5083 | 1.0 | 1 | 6.17 |
| CHEMBL3747647 | — | — | 1 | 5.75 |
| CHEMBL3746353 | — | — | 1 | 5.37 |
| CHEMBL3746912 | — | — | 1 | 5.21 |
| CHEMBL3696896 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3747448 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3747513 | CB-5083 | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL3747647 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL3746353 | — | IC50 | = | 4240.0 | nM | 5.37 |
| CHEMBL3746912 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL3696896 | — | IC50 | = | 15320.0 | nM | 4.82 |