Assay Detail
Binding
CHEMBL3748824
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Inhibition of EML4-ALK L1152R 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 | 6.28 | 6.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3747134 | — | — | 1 | 6.78 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 6.77 |
| CHEMBL3735401 | — | — | 1 | 6.71 |
| CHEMBL3747267 | — | — | 1 | 6.66 |
| CHEMBL3746482 | — | — | 1 | 6.55 |
| CHEMBL3746678 | — | — | 1 | 6.54 |
| CHEMBL3736273 | — | — | 1 | 6.53 |
| CHEMBL3747611 | — | — | 1 | 6.46 |
| CHEMBL3746395 | — | — | 1 | 6.46 |
| CHEMBL3746522 | — | — | 1 | 6.26 |
| CHEMBL3746960 | — | — | 1 | 6.21 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.19 |
| CHEMBL3746665 | — | — | 1 | 6.16 |
| CHEMBL3747108 | — | — | 1 | 6.15 |
| CHEMBL3734844 | — | — | 1 | 6.11 |
| CHEMBL3397300 | — | — | 1 | 5.64 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.56 |
| CHEMBL3747406 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3747134 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL1738797 | ALECTINIB | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL3735401 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL3747267 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3746482 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL3746678 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL3736273 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL3747611 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL3746395 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL3746522 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL3746960 | — | IC50 | = | 617.0 | nM | 6.21 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL3746665 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL3747108 | — | IC50 | = | 711.0 | nM | 6.15 |
| CHEMBL3734844 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL3397300 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 2747.0 | nM | 5.56 |
| CHEMBL3747406 | — | IC50 | = | 5750.0 | nM | 5.24 |