Assay Detail
Binding
CHEMBL3815445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M double mutant (unknown origin) expressed in mouse BaF/3 cells assessed as cell growth inhibition after 72 hrs by MTS assay
4
Total Activities
4
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
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.71 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814940 | — | — | 1 | 5.75 |
| CHEMBL3814021 | — | — | 1 | 5.69 |
| CHEMBL3814846 | — | — | 1 | 5.68 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814940 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL3814021 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL3814846 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL939 | GEFITINIB | IC50 | > | 10000.0 | nM | - |