Assay Detail
Binding
CHEMBL2427714
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.00 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.24 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 9.20 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.23 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.06 |
| CHEMBL2426279 | — | — | 1 | 7.77 |
| CHEMBL2426278 | — | — | 1 | 7.64 |
| CHEMBL2426282 | — | — | 1 | 7.54 |
| CHEMBL1229592 | — | — | 1 | 7.36 |
| CHEMBL2426287 | — | — | 1 | 7.07 |
| CHEMBL2424676 | — | — | 1 | 6.85 |
| CHEMBL2426277 | — | — | 1 | 6.85 |
| CHEMBL2426286 | — | — | 1 | 6.82 |
| CHEMBL2426377 | — | — | 1 | 6.60 |
| CHEMBL2426281 | — | — | 1 | 6.57 |
| CHEMBL2426290 | — | — | 1 | 6.42 |
| CHEMBL2426289 | — | — | 1 | 6.41 |
| CHEMBL2426288 | — | — | 1 | 6.40 |
| CHEMBL2426378 | — | — | 1 | 5.89 |
| CHEMBL2426285 | — | — | 1 | 5.75 |
| CHEMBL2426284 | — | — | 1 | 5.55 |
| CHEMBL2426283 | — | — | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL939 | GEFITINIB | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL2426279 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2426278 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2426282 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1229592 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2426287 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2424676 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2426277 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2426286 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2426377 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2426281 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2426290 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2426289 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2426288 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2426378 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2426285 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2426284 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2426283 | — | IC50 | = | 19000.0 | nM | 4.72 |