Assay Detail
Functional
CHEMBL3815448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against gefitinib-resistant human PC9/GR4 cells expressing Del19/T790M double mutant assessed as cell viability after 72 hrs by cell titer-glo luminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PC9/GR4 |
| Confidence | 1 — Organism |
| 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 | 6 | 5.06 | 5.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814021 | — | — | 1 | 5.67 |
| CHEMBL3814940 | — | — | 1 | 5.24 |
| CHEMBL3814846 | — | — | 1 | 5.08 |
| CHEMBL3814257 | — | — | 1 | 4.90 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 4.79 |
| CHEMBL3814211 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814021 | — | IC50 | = | 2157.0 | nM | 5.67 |
| CHEMBL3814940 | — | IC50 | = | 5701.0 | nM | 5.24 |
| CHEMBL3814846 | — | IC50 | = | 8313.0 | nM | 5.08 |
| CHEMBL3814257 | — | IC50 | = | 12620.0 | nM | 4.90 |
| CHEMBL939 | GEFITINIB | IC50 | = | 16330.0 | nM | 4.79 |
| CHEMBL3814211 | — | IC50 | = | 21700.0 | nM | 4.66 |