Assay Detail
Functional
CHEMBL4362852
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H2228 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel derivatives of anaplastic lymphoma kinase inhibitors: Synthesis, radiolabeling, and preliminary biological studies of fluoroethyl analogues of crizotinib, alectinib, and ceritinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.17 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 8.19 |
| CHEMBL4474454 | — | — | 1 | 8.00 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.55 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.54 |
| CHEMBL4566676 | — | — | 1 | 5.12 |
| CHEMBL4532807 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738797 | ALECTINIB | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4474454 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4566676 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4532807 | — | IC50 | = | 24200.0 | nM | 4.62 |