Assay Detail
Binding
CHEMBL5710049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CD74-ROS1 expressed in mouse BaF3 cells assessed as inhibition of phosphorylated ROS1 incubated for 1 hr by ELISA analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
H-2 class II histocompatibility antigen gamma chain/Proto-oncogene tyrosine-protein kinase ROS (CHEMBL6066844) ↗| Type | CHIMERIC PROTEIN |
| Organism | Mus musculus |
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 | 6 | 8.49 | 9.64 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0003060 |
| EFO_TERM | EFO_TERM | - | — | non-small cell lung carcinoma |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5712062 | — | — | 1 | 9.64 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.82 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.42 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.41 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.15 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5712062 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1738797 | ALECTINIB | IC50 | > | 10000.0 | nM | - |