Assay Detail
Binding
CHEMBL5663121
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Inhibition of EGFR expressed in mouse NIH3T3 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.15 | 8.80 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0003060 |
| EFO_TERM | EFO_TERM | - | — | non-small cell lung carcinoma |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.80 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.24 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.84 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL939 | GEFITINIB | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 19.3 | nM | 7.71 |