Assay Detail
Binding
CHEMBL4828947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ALK L1196M mutant (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.70 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 9.60 |
| CHEMBL4855319 | — | — | 1 | 8.77 |
| CHEMBL4849606 | — | — | 1 | 8.62 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.80 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | - |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403108 | CERITINIB | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4855319 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4849606 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | - | — | - | |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - |