Assay Detail
Binding
CHEMBL4382301
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Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
16
Total Activities
16
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 | 16 | 7.53 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448107 | — | — | 1 | 8.70 |
| CHEMBL4473365 | — | — | 1 | 8.40 |
| CHEMBL4449391 | — | — | 1 | 8.40 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.22 |
| CHEMBL4565984 | — | — | 1 | 8.10 |
| CHEMBL4531697 | — | — | 1 | 7.72 |
| CHEMBL4540442 | — | — | 1 | 7.72 |
| CHEMBL4467561 | — | — | 1 | 7.72 |
| CHEMBL4520341 | — | — | 1 | 7.68 |
| CHEMBL4581316 | — | — | 1 | 7.64 |
| CHEMBL1229592 | — | — | 1 | 7.58 |
| CHEMBL4558227 | — | — | 1 | 7.17 |
| CHEMBL4516287 | — | — | 1 | 7.11 |
| CHEMBL4465103 | — | — | 1 | 6.63 |
| CHEMBL4533742 | — | — | 1 | 6.18 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448107 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4473365 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4449391 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3353410 | OSIMERTINIB | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4565984 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4531697 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4540442 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4467561 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4520341 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4581316 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1229592 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4558227 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4516287 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4465103 | — | EC50 | = | 236.0 | nM | 6.63 |
| CHEMBL4533742 | — | EC50 | = | 666.0 | nM | 6.18 |
| CHEMBL2403108 | CERITINIB | EC50 | = | 3000.0 | nM | 5.52 |