Assay Detail
Functional
CHEMBL4828951
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Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
5
Total Activities
5
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
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.23 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4855319 | — | — | 1 | 6.89 |
| CHEMBL4849606 | — | — | 1 | 6.75 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.70 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.58 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4855319 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4849606 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - |