Assay Detail
Functional
CHEMBL4400317
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A549 cells harbouring EGFR G1202R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
36
Total Activities
36
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
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 | 36 | 6.07 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4562805 | — | — | 1 | 7.52 |
| CHEMBL4536955 | — | — | 1 | 6.77 |
| CHEMBL4546844 | — | — | 1 | 6.72 |
| CHEMBL4468370 | — | — | 1 | 6.57 |
| CHEMBL4448400 | — | — | 1 | 6.44 |
| CHEMBL4471142 | — | — | 1 | 6.39 |
| CHEMBL4460117 | — | — | 1 | 6.36 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.29 |
| CHEMBL4434682 | — | — | 1 | 6.21 |
| CHEMBL4461807 | — | — | 1 | 6.19 |
| CHEMBL4592055 | — | — | 1 | 6.15 |
| CHEMBL4452164 | — | — | 1 | 6.13 |
| CHEMBL4531143 | — | — | 1 | 6.03 |
| CHEMBL4462528 | — | — | 1 | 6.03 |
| CHEMBL4483504 | — | — | 1 | 6.01 |
| CHEMBL4566617 | — | — | 1 | 6.01 |
| CHEMBL4592666 | — | — | 1 | 5.99 |
| CHEMBL4459181 | — | — | 1 | 5.99 |
| CHEMBL4572661 | — | — | 1 | 5.97 |
| CHEMBL4462608 | — | — | 1 | 5.97 |
| CHEMBL4519461 | — | — | 1 | 5.96 |
| CHEMBL4457180 | — | — | 1 | 5.96 |
| CHEMBL4449742 | — | — | 1 | 5.94 |
| CHEMBL4516260 | — | — | 1 | 5.93 |
| CHEMBL4515407 | — | — | 1 | 5.91 |
| CHEMBL4436697 | — | — | 1 | 5.90 |
| CHEMBL4446022 | — | — | 1 | 5.86 |
| CHEMBL4471628 | — | — | 1 | 5.83 |
| CHEMBL4580622 | — | — | 1 | 5.81 |
| CHEMBL4454973 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4562805 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4536955 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4546844 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4468370 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4448400 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4471142 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4460117 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4434682 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4461807 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4592055 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4452164 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4531143 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4462528 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4566617 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4483504 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4592666 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4459181 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4572661 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4462608 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4519461 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL4457180 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4449742 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4516260 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4515407 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4436697 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4446022 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4471628 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4580622 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4454973 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL4540084 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4473400 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL4569983 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4467298 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4444127 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4573678 | — | IC50 | = | 3130.0 | nM | 5.50 |