Assay Detail
Binding
CHEMBL5710014
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Binding affinity to recombinant human ROS1 assessed as inhibition constant in presence of ATP by microfluidic mobility shift assay
5
Total Activities
5
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase ROS (CHEMBL5568) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| Ki | 5 | 8.02 | 9.22 |
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 |
|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 9.22 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 9.15 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.09 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 5.62 |
| CHEMBL5712062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2403108 | CERITINIB | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL1230609 | FORETINIB | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL1738797 | ALECTINIB | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL5712062 | — | Ki | < | 0.025 | nM | - |