Assay Detail
Binding
CHEMBL4324123
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Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 7.61 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537790 | — | — | 1 | 9.70 |
| CHEMBL4562138 | — | — | 1 | 9.00 |
| CHEMBL4550104 | — | — | 1 | 8.30 |
| CHEMBL4566193 | — | — | 1 | 8.22 |
| CHEMBL4519157 | — | — | 1 | 7.57 |
| CHEMBL4532034 | — | — | 1 | 7.29 |
| CHEMBL4434788 | — | — | 1 | 6.82 |
| CHEMBL4449589 | — | — | 1 | 6.57 |
| CHEMBL4525935 | — | — | 1 | 6.48 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.11 |
| CHEMBL4591327 | — | — | 1 | - |
| CHEMBL4444231 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537790 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4562138 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4550104 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4566193 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4519157 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4532034 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4434788 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4449589 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4525935 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4591327 | — | IC50 | - | — | - | |
| CHEMBL4444231 | — | IC50 | - | — | - |