Assay Detail
Binding
CHEMBL4324122
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Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
12
Total Activities
12
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
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.02 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537790 | — | — | 1 | 9.22 |
| CHEMBL4562138 | — | — | 1 | 9.10 |
| CHEMBL4550104 | — | — | 1 | 9.00 |
| CHEMBL4532034 | — | — | 1 | 9.00 |
| CHEMBL4566193 | — | — | 1 | 8.92 |
| CHEMBL4519157 | — | — | 1 | 8.52 |
| CHEMBL4434788 | — | — | 1 | 7.66 |
| CHEMBL4449589 | — | — | 1 | 7.46 |
| CHEMBL4525935 | — | — | 1 | 7.37 |
| CHEMBL4591327 | — | — | 1 | 6.10 |
| CHEMBL4444231 | — | — | 1 | 5.85 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537790 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4562138 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4550104 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4532034 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4566193 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4519157 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4434788 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4449589 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4525935 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4591327 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4444231 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 3100.0 | nM | - |