Assay Detail
Binding
CHEMBL4400323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain G1202R mutant using srctide as substrate incubated for 1 hr by mobility shift assay
8
Total Activities
8
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
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.90 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4562805 | — | — | 1 | 8.37 |
| CHEMBL4468370 | — | — | 1 | 8.20 |
| CHEMBL4448400 | — | — | 1 | 8.15 |
| CHEMBL4546844 | — | — | 1 | 8.03 |
| CHEMBL4536955 | — | — | 1 | 7.99 |
| CHEMBL4462528 | — | — | 1 | 7.94 |
| CHEMBL4471142 | — | — | 1 | 7.80 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4562805 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4468370 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4448400 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4546844 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4536955 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4462528 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4471142 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 197.0 | nM | 6.71 |