Assay Detail
Binding
CHEMBL3748825
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Inhibition of EML4-ALK 1151Tins 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 | 0 — Uncurated / Unknown |
| 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 | 6.56 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3746665 | — | — | 1 | 7.28 |
| CHEMBL3746678 | — | — | 1 | 7.17 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 7.14 |
| CHEMBL3746522 | — | — | 1 | 7.11 |
| CHEMBL3735401 | — | — | 1 | 6.97 |
| CHEMBL3747267 | — | — | 1 | 6.94 |
| CHEMBL3397300 | — | — | 1 | 6.85 |
| CHEMBL3736273 | — | — | 1 | 6.79 |
| CHEMBL3746960 | — | — | 1 | 6.69 |
| CHEMBL3747134 | — | — | 1 | 6.54 |
| CHEMBL3746482 | — | — | 1 | 6.42 |
| CHEMBL3734844 | — | — | 1 | 6.21 |
| CHEMBL3747108 | — | — | 1 | 6.20 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.17 |
| CHEMBL3747611 | — | — | 1 | 6.09 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.07 |
| CHEMBL3746395 | — | — | 1 | 6.03 |
| CHEMBL3747406 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3746665 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3746678 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1738797 | ALECTINIB | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3746522 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3735401 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3747267 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3397300 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL3736273 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL3746960 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL3747134 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL3746482 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL3734844 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3747108 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL3747611 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 857.0 | nM | 6.07 |
| CHEMBL3746395 | — | IC50 | = | 925.0 | nM | 6.03 |
| CHEMBL3747406 | — | IC50 | = | 4409.0 | nM | 5.36 |