Assay Detail
Functional
CHEMBL5710055
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Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC78 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.66 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5712062 | — | — | 1 | 8.94 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.72 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.68 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.30 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5712062 | — | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL1738797 | ALECTINIB | IC50 | > | 10000.0 | nM | - |