Assay Detail
Binding
CHEMBL4266247
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Inhibition of wild type EML4/ALK (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 | 8.38 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4286522 | — | — | 1 | 9.15 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 8.89 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4286522 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3286830 | LORLATINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 80.0 | nM | 7.10 |