Assay Detail
Binding
CHEMBL3993015
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Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay
19
Total Activities
19
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 | 19 | 8.39 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099660 | — | — | 1 | 8.89 |
| CHEMBL4078406 | — | — | 1 | 8.85 |
| CHEMBL4105099 | — | — | 1 | 8.82 |
| CHEMBL4080869 | — | — | 1 | 8.80 |
| CHEMBL4081656 | — | — | 1 | 8.77 |
| CHEMBL4089672 | — | — | 1 | 8.77 |
| CHEMBL4091928 | — | — | 1 | 8.72 |
| CHEMBL4070217 | — | — | 1 | 8.68 |
| CHEMBL4097392 | — | — | 1 | 8.68 |
| CHEMBL4067503 | — | — | 1 | 8.66 |
| CHEMBL4096452 | — | — | 1 | 8.60 |
| CHEMBL4088751 | — | — | 1 | 8.55 |
| CHEMBL4062466 | — | — | 1 | 8.47 |
| CHEMBL4084168 | — | — | 1 | 8.44 |
| CHEMBL4071105 | — | — | 1 | 8.36 |
| CHEMBL4061549 | — | — | 1 | 8.21 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.54 |
| CHEMBL4089527 | — | — | 1 | 7.44 |
| CHEMBL4061375 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099660 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4078406 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4105099 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4080869 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4081656 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4089672 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4091928 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4070217 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4097392 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4067503 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4096452 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4088751 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4062466 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4084168 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4071105 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4061549 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4089527 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4061375 | — | IC50 | = | 570.0 | nM | 6.24 |