Assay Detail
Binding
CHEMBL4267882
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Dual potent ALK and ROS1 inhibitors combating drug-resistant mutants: Synthesis and biological evaluation of aminopyridine-containing diarylaminopyrimidine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.46 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4277936 | — | — | 1 | 5.89 |
| CHEMBL4284800 | — | — | 1 | 5.80 |
| CHEMBL4281394 | — | — | 1 | 5.70 |
| CHEMBL4291608 | — | — | 1 | 5.66 |
| CHEMBL4285785 | — | — | 1 | 5.41 |
| CHEMBL4279793 | — | — | 1 | 5.32 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 4.46 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4277936 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4284800 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4281394 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4291608 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4285785 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4279793 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 380000.0 | nM | - |