Assay Detail
Binding
CHEMBL4266252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.20 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4286522 | — | — | 1 | 7.85 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 7.68 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4286522 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3286830 | LORLATINIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 843.0 | nM | 6.07 |