Assay Detail
Binding
CHEMBL4821238
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR (unknown origin)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.55 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603266 | — | — | 1 | 9.44 |
| CHEMBL4858583 | — | — | 1 | 9.41 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.22 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.00 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.89 |
| CHEMBL250318 | — | — | 1 | 7.85 |
| CHEMBL4856453 | — | — | 1 | 7.48 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.26 |
| CHEMBL4866476 | — | — | 1 | 7.18 |
| CHEMBL4857477 | — | — | 1 | 7.09 |
| CHEMBL1988225 | — | — | 1 | 7.09 |
| CHEMBL4849859 | — | — | 1 | 6.87 |
| CHEMBL4859473 | — | — | 1 | 6.84 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.78 |
| CHEMBL4877452 | — | — | 1 | 6.75 |
| CHEMBL210378 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603266 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4858583 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 12.92 | nM | 7.89 |
| CHEMBL250318 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4856453 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 54.34 | nM | 7.26 |
| CHEMBL4866476 | — | IC50 | = | 65.63 | nM | 7.18 |
| CHEMBL4857477 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1988225 | — | IC50 | = | 81.07 | nM | 7.09 |
| CHEMBL4849859 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4859473 | — | IC50 | = | 143.4 | nM | 6.84 |
| CHEMBL939 | GEFITINIB | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4877452 | — | IC50 | = | 178.1 | nM | 6.75 |
| CHEMBL210378 | — | IC50 | = | 204.0 | nM | 6.69 |