Assay Detail
Binding
CHEMBL4136449
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay
10
Total Activities
10
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
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.25 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4174347 | — | — | 1 | 8.96 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 8.70 |
| CHEMBL4166436 | — | — | 1 | 8.52 |
| CHEMBL4168473 | — | — | 1 | 8.34 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.17 |
| CHEMBL4166038 | — | — | 1 | 8.10 |
| CHEMBL4159161 | — | — | 1 | 8.07 |
| CHEMBL4167072 | — | — | 1 | 8.01 |
| CHEMBL4160581 | — | — | 1 | 7.87 |
| CHEMBL4163707 | — | — | 1 | 7.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4174347 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4166436 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4168473 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4166038 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4159161 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4167072 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4160581 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4163707 | — | IC50 | = | 19.3 | nM | 7.71 |