Assay Detail
Binding
CHEMBL4348478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in Baculovirus expression system using IRS1 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 |
Target
Proto-oncogene tyrosine-protein kinase ROS (CHEMBL5568) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.71 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470529 | — | — | 1 | 9.37 |
| CHEMBL4573193 | — | — | 1 | 9.12 |
| CHEMBL4447747 | — | — | 1 | 9.09 |
| CHEMBL4519408 | — | — | 1 | 9.01 |
| CHEMBL4464571 | — | — | 1 | 8.77 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 8.51 |
| CHEMBL4466920 | — | — | 1 | 8.28 |
| CHEMBL4465558 | — | — | 1 | 8.17 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470529 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4573193 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL4447747 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4519408 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL4464571 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4466920 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4465558 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 9.3 | nM | 8.03 |