Assay Detail
Binding
CHEMBL4332363
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin peptide as substrate measured after 10 mins by HTRF assay
9
Total Activities
9
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
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.65 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4473875 | — | — | 1 | 9.16 |
| CHEMBL4474073 | — | — | 1 | 9.12 |
| CHEMBL4577883 | — | — | 1 | 9.03 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.02 |
| CHEMBL4591886 | — | — | 1 | 8.83 |
| CHEMBL4450824 | — | — | 1 | 8.81 |
| CHEMBL4443188 | — | — | 1 | 8.56 |
| CHEMBL4592101 | — | — | 1 | 8.55 |
| CHEMBL4447976 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4473875 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4474073 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL4577883 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL4591886 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL4450824 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL4443188 | — | IC50 | = | 2.73 | nM | 8.56 |
| CHEMBL4592101 | — | IC50 | = | 2.84 | nM | 8.55 |
| CHEMBL4447976 | — | IC50 | = | 153.5 | nM | 6.81 |