Assay Detail
Binding
CHEMBL4668374
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ROS1 L2026M mutant (unknown origin) in presence of ATP by microfluidic mobility shift assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
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
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 9.12 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 10.00 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286830 | LORLATINIB | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL601719 | CRIZOTINIB | Ki | = | 5.8 | nM | 8.24 |