Assay Detail
Binding
CHEMBL3831013
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Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H3122 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.25 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3735648 | — | — | 1 | 7.75 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 7.72 |
| CHEMBL3735386 | — | — | 1 | 7.31 |
| CHEMBL3736388 | — | — | 1 | 6.90 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3735648 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL1738797 | ALECTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3735386 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3736388 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 261.0 | nM | 6.58 |