Assay Detail
Binding
CHEMBL4348492
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay
9
Total Activities
9
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
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.75 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470529 | — | — | 1 | 8.17 |
| CHEMBL4573193 | — | — | 1 | 8.07 |
| CHEMBL4447747 | — | — | 1 | 7.99 |
| CHEMBL4466920 | — | — | 1 | 7.92 |
| CHEMBL4464571 | — | — | 1 | 7.81 |
| CHEMBL4465558 | — | — | 1 | 7.70 |
| CHEMBL4519408 | — | — | 1 | 7.63 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.70 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470529 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4573193 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4447747 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4466920 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL4464571 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL4465558 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL4519408 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL601719 | CRIZOTINIB | IC50 | > | 1000.0 | nM | - |