Assay Detail
Functional
CHEMBL4136442
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK 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 | NCI-H2228 |
| 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 | 6.67 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166436 | — | — | 1 | 7.10 |
| CHEMBL4166038 | — | — | 1 | 7.06 |
| CHEMBL4160581 | — | — | 1 | 7.05 |
| CHEMBL4174347 | — | — | 1 | 7.02 |
| CHEMBL4167072 | — | — | 1 | 7.01 |
| CHEMBL4163707 | — | — | 1 | 7.00 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.00 |
| CHEMBL4171597 | — | — | 1 | 6.89 |
| CHEMBL4159204 | — | — | 1 | 6.82 |
| CHEMBL4160984 | — | — | 1 | 6.75 |
| CHEMBL4168473 | — | — | 1 | 6.72 |
| CHEMBL4176500 | — | — | 1 | 6.70 |
| CHEMBL4175040 | — | — | 1 | 6.64 |
| CHEMBL4177273 | — | — | 1 | 6.64 |
| CHEMBL4159161 | — | — | 1 | 6.64 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.62 |
| CHEMBL4159487 | — | — | 1 | 6.55 |
| CHEMBL4176649 | — | — | 1 | 6.54 |
| CHEMBL4169421 | — | — | 1 | 6.52 |
| CHEMBL4159911 | — | — | 1 | 6.52 |
| CHEMBL4175110 | — | — | 1 | 6.51 |
| CHEMBL4164390 | — | — | 1 | 6.47 |
| CHEMBL4167712 | — | — | 1 | 6.46 |
| CHEMBL4173922 | — | — | 1 | 6.46 |
| CHEMBL4162551 | — | — | 1 | 6.46 |
| CHEMBL4163835 | — | — | 1 | 6.43 |
| CHEMBL4168642 | — | — | 1 | 6.42 |
| CHEMBL4177168 | — | — | 1 | 6.39 |
| CHEMBL4164810 | — | — | 1 | 6.32 |
| CHEMBL4170486 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166436 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4166038 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4160581 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4174347 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4167072 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4163707 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4171597 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4159204 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4160984 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4168473 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4176500 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4175040 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4177273 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4159161 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4159487 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4176649 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4169421 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4159911 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4175110 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4164390 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4167712 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4173922 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4162551 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4163835 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4168642 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4177168 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4164810 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4170486 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4164963 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4160337 | — | IC50 | > | 1000.0 | nM | - |