Assay Detail
Functional
CHEMBL4348488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 1 — Organism |
| 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 | 30 | 6.05 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470529 | — | — | 1 | 7.14 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.09 |
| CHEMBL4447747 | — | — | 1 | 7.03 |
| CHEMBL4465558 | — | — | 1 | 7.00 |
| CHEMBL4573193 | — | — | 1 | 6.96 |
| CHEMBL4590579 | — | — | 1 | 6.85 |
| CHEMBL4456914 | — | — | 1 | 6.01 |
| CHEMBL4452463 | — | — | 1 | 5.99 |
| CHEMBL4518307 | — | — | 1 | 5.97 |
| CHEMBL4554640 | — | — | 1 | 5.96 |
| CHEMBL4450345 | — | — | 1 | 5.94 |
| CHEMBL4558432 | — | — | 1 | 5.94 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.93 |
| CHEMBL4519408 | — | — | 1 | 5.91 |
| CHEMBL4554368 | — | — | 1 | 5.90 |
| CHEMBL4461727 | — | — | 1 | 5.85 |
| CHEMBL4463949 | — | — | 1 | 5.83 |
| CHEMBL4437160 | — | — | 1 | 5.76 |
| CHEMBL4456460 | — | — | 1 | 5.74 |
| CHEMBL4466920 | — | — | 1 | 5.70 |
| CHEMBL4575542 | — | — | 1 | 5.68 |
| CHEMBL4437262 | — | — | 1 | 5.66 |
| CHEMBL4557617 | — | — | 1 | 5.63 |
| CHEMBL4519546 | — | — | 1 | 5.62 |
| CHEMBL4473467 | — | — | 1 | 5.62 |
| CHEMBL4586917 | — | — | 1 | 5.61 |
| CHEMBL4472611 | — | — | 1 | 5.55 |
| CHEMBL4464571 | — | — | 1 | 5.45 |
| CHEMBL4523049 | — | — | 1 | - |
| CHEMBL4445053 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470529 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4447747 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4465558 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4573193 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4590579 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4456914 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4452463 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4518307 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4554640 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4450345 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4558432 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4519408 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4554368 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4461727 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4463949 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4437160 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL4456460 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4466920 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4575542 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL4437262 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4557617 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4519546 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4473467 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL4586917 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL4472611 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL4464571 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL4523049 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4445053 | — | IC50 | > | 5000.0 | nM | - |