Assay Detail
Binding
CHEMBL4382302
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Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent dual ALK and EGFR T790M inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.35 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448107 | — | — | 1 | 8.30 |
| CHEMBL4473365 | — | — | 1 | 8.22 |
| CHEMBL4565984 | — | — | 1 | 8.22 |
| CHEMBL4449391 | — | — | 1 | 8.22 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.75 |
| CHEMBL4540442 | — | — | 1 | 7.68 |
| CHEMBL4467561 | — | — | 1 | 7.62 |
| CHEMBL4520341 | — | — | 1 | 7.36 |
| CHEMBL4531697 | — | — | 1 | 7.33 |
| CHEMBL1229592 | — | — | 1 | 7.17 |
| CHEMBL4581316 | — | — | 1 | 7.08 |
| CHEMBL4558227 | — | — | 1 | 6.80 |
| CHEMBL4516287 | — | — | 1 | 6.71 |
| CHEMBL4465103 | — | — | 1 | 6.17 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448107 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4473365 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4565984 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4449391 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3353410 | OSIMERTINIB | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4540442 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4467561 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4520341 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4531697 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1229592 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4581316 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4558227 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4516287 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4465103 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL2403108 | CERITINIB | EC50 | = | 2500.0 | nM | 5.60 |