Assay Detail
Binding
CHEMBL3993020
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Inhibition of ALK G1269A mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay
2
Total Activities
2
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
Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 9.13 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099660 | — | — | 1 | 9.40 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 8.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099660 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 1.4 | nM | 8.85 |