Assay Detail
Functional
CHEMBL4136443
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC78 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.56 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4174347 | — | — | 1 | 7.40 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.24 |
| CHEMBL4166038 | — | — | 1 | 7.09 |
| CHEMBL4167072 | — | — | 1 | 7.03 |
| CHEMBL4166436 | — | — | 1 | 7.02 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.77 |
| CHEMBL4176500 | — | — | 1 | 6.75 |
| CHEMBL4159204 | — | — | 1 | 6.62 |
| CHEMBL4177168 | — | — | 1 | 6.57 |
| CHEMBL4168473 | — | — | 1 | 6.50 |
| CHEMBL4159911 | — | — | 1 | 6.48 |
| CHEMBL4175110 | — | — | 1 | 6.46 |
| CHEMBL4159161 | — | — | 1 | 6.42 |
| CHEMBL4164810 | — | — | 1 | 6.42 |
| CHEMBL4160984 | — | — | 1 | 6.37 |
| CHEMBL4175040 | — | — | 1 | 6.33 |
| CHEMBL4171597 | — | — | 1 | 6.31 |
| CHEMBL4168642 | — | — | 1 | 6.28 |
| CHEMBL4176649 | — | — | 1 | 6.28 |
| CHEMBL4160581 | — | — | 1 | 6.24 |
| CHEMBL4164390 | — | — | 1 | 6.11 |
| CHEMBL4163707 | — | — | 1 | 6.09 |
| CHEMBL4170486 | — | — | 1 | 6.04 |
| CHEMBL4164963 | — | — | 1 | - |
| CHEMBL4169421 | — | — | 1 | - |
| CHEMBL4160337 | — | — | 1 | - |
| CHEMBL4173922 | — | — | 1 | - |
| CHEMBL4159487 | — | — | 1 | - |
| CHEMBL4163835 | — | — | 1 | - |
| CHEMBL4162551 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4174347 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4166038 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4167072 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4166436 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4176500 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4159204 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4177168 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4168473 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4159911 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4175110 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4159161 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4164810 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4160984 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4175040 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4171597 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4168642 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4176649 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4160581 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4164390 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4163707 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4170486 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4164963 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4169421 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4160337 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4173922 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4159487 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4163835 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4162551 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4177273 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4167712 | — | IC50 | > | 1000.0 | nM | - |