Assay Detail
Binding
CHEMBL3748821
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Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 8.70 |
| CHEMBL3746665 | — | — | 1 | 8.70 |
| CHEMBL3735401 | — | — | 1 | 8.70 |
| CHEMBL3397300 | — | — | 1 | 8.52 |
| CHEMBL3746678 | — | — | 1 | 8.10 |
| CHEMBL3746960 | — | — | 1 | 8.05 |
| CHEMBL3747267 | — | — | 1 | 7.92 |
| CHEMBL3736273 | — | — | 1 | 7.62 |
| CHEMBL3746522 | — | — | 1 | 7.62 |
| CHEMBL3734844 | — | — | 1 | 7.24 |
| CHEMBL3747108 | — | — | 1 | 7.24 |
| CHEMBL3746482 | — | — | 1 | 7.23 |
| CHEMBL3747134 | — | — | 1 | 7.04 |
| CHEMBL3746395 | — | — | 1 | 6.94 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.84 |
| CHEMBL3747406 | — | — | 1 | 6.82 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.79 |
| CHEMBL3747611 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738797 | ALECTINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3746665 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3735401 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3397300 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3746678 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3746960 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3747267 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3736273 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3746522 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3734844 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3747108 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3746482 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3747134 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3746395 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3747406 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3747611 | — | IC50 | = | 177.0 | nM | 6.75 |