Assay Detail
Binding
CHEMBL4628613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 40 mins in presence of ATP by caliper mobility shift assay
7
Total Activities
7
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 and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.33 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.00 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.00 |
| CHEMBL4643111 | — | — | 1 | 8.22 |
| CHEMBL2441563 | — | — | 1 | 8.15 |
| CHEMBL4635100 | — | — | 1 | 8.15 |
| CHEMBL4648271 | — | — | 1 | 8.10 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4643111 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2441563 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4635100 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4648271 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL554 | LAPATINIB | IC50 | = | 22.0 | nM | 7.66 |