Assay Detail
Binding
CHEMBL2444968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type EGFR in human A431 cells assessed as growth inhibition after 48 hrs by MTT assay
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 10 | - | - |
| IC50 | 4 | 5.70 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441567 | — | — | 1 | 6.05 |
| CHEMBL2441565 | — | — | 1 | 5.66 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.40 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL2441566 | — | — | 1 | - |
| CHEMBL2441564 | — | — | 1 | - |
| CHEMBL2441563 | — | — | 1 | - |
| CHEMBL2441562 | — | — | 1 | - |
| CHEMBL2441561 | — | — | 1 | - |
| CHEMBL2441560 | — | — | 1 | - |
| CHEMBL2441559 | — | — | 1 | - |
| CHEMBL2441558 | — | — | 1 | - |
| CHEMBL2441557 | — | — | 1 | - |
| CHEMBL2441568 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441567 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2441565 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL939 | GEFITINIB | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL31965 | CANERTINIB | Inhibition | - | % | - | |
| CHEMBL2441566 | — | Inhibition | - | % | - | |
| CHEMBL2441564 | — | Inhibition | - | % | - | |
| CHEMBL2441563 | — | Inhibition | - | % | - | |
| CHEMBL2441562 | — | Inhibition | - | % | - | |
| CHEMBL2441561 | — | Inhibition | - | % | - | |
| CHEMBL2441560 | — | Inhibition | - | % | - | |
| CHEMBL2441559 | — | Inhibition | - | % | - | |
| CHEMBL2441558 | — | Inhibition | - | % | - | |
| CHEMBL2441557 | — | Inhibition | - | % | - | |
| CHEMBL2441568 | — | IC50 | > | 30000.0 | nM | - |