Assay Detail
Binding
CHEMBL5147203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of his-GST tagged human EGFR L858R/T790M double mutant expressed in insect cells incubated for 30 mins in presence of ATP by HTRF kinase assay
29
Total Activities
29
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
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.84 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196360 | — | — | 1 | 10.00 |
| CHEMBL5201543 | — | — | 1 | 10.00 |
| CHEMBL5182553 | — | — | 1 | 9.70 |
| CHEMBL5206902 | — | — | 1 | 9.70 |
| CHEMBL4443062 | — | — | 1 | 9.52 |
| CHEMBL5191510 | — | — | 1 | 9.52 |
| CHEMBL5177272 | — | — | 1 | 9.22 |
| CHEMBL5191674 | — | — | 1 | 9.22 |
| CHEMBL5177306 | — | — | 1 | 9.05 |
| CHEMBL5198812 | — | — | 1 | 9.05 |
| CHEMBL5172573 | — | — | 1 | 9.05 |
| CHEMBL5202129 | — | — | 1 | 8.96 |
| CHEMBL5197154 | — | — | 1 | 8.92 |
| CHEMBL5178571 | — | — | 1 | 8.85 |
| CHEMBL5173701 | — | — | 1 | 8.74 |
| CHEMBL5176460 | — | — | 1 | 8.74 |
| CHEMBL5207108 | — | — | 1 | 8.72 |
| CHEMBL5200637 | — | — | 1 | 8.66 |
| CHEMBL5204970 | — | — | 1 | 8.51 |
| CHEMBL5195912 | — | — | 1 | 8.49 |
| CHEMBL4214567 | — | — | 1 | 8.48 |
| CHEMBL5178865 | — | — | 1 | 8.47 |
| CHEMBL5178754 | — | — | 1 | 8.40 |
| CHEMBL5208065 | — | — | 1 | 8.30 |
| CHEMBL5204270 | — | — | 1 | 8.24 |
| CHEMBL5187605 | — | — | 1 | 8.17 |
| CHEMBL5200988 | — | — | 1 | 8.01 |
| CHEMBL5206436 | — | — | 1 | 7.99 |
| CHEMBL5207462 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196360 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5201543 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5182553 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5206902 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4443062 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5191510 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5177272 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5191674 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5177306 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5198812 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5172573 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5202129 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5197154 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5178571 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5173701 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5176460 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5207108 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5200637 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5204970 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5195912 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4214567 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5178865 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5178754 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5208065 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5204270 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5187605 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5200988 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5206436 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL5207462 | — | IC50 | = | 17.8 | nM | 7.75 |