Assay Detail
Functional
CHEMBL5147205
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| 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 | 7.24 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196360 | — | — | 1 | 8.52 |
| CHEMBL5191510 | — | — | 1 | 8.22 |
| CHEMBL5201543 | — | — | 1 | 8.22 |
| CHEMBL5206902 | — | — | 1 | 8.15 |
| CHEMBL5177272 | — | — | 1 | 8.00 |
| CHEMBL5191674 | — | — | 1 | 7.80 |
| CHEMBL5182553 | — | — | 1 | 7.70 |
| CHEMBL5198812 | — | — | 1 | 7.70 |
| CHEMBL4443062 | — | — | 1 | 7.68 |
| CHEMBL5172573 | — | — | 1 | 7.68 |
| CHEMBL5207108 | — | — | 1 | 7.64 |
| CHEMBL5197154 | — | — | 1 | 7.62 |
| CHEMBL5177306 | — | — | 1 | 7.37 |
| CHEMBL5176460 | — | — | 1 | 7.36 |
| CHEMBL5208065 | — | — | 1 | 7.36 |
| CHEMBL5178865 | — | — | 1 | 7.21 |
| CHEMBL5173701 | — | — | 1 | 7.16 |
| CHEMBL5178571 | — | — | 1 | 7.14 |
| CHEMBL5195912 | — | — | 1 | 7.00 |
| CHEMBL5187605 | — | — | 1 | 6.90 |
| CHEMBL5178754 | — | — | 1 | 6.68 |
| CHEMBL4214567 | — | — | 1 | 6.66 |
| CHEMBL5204270 | — | — | 1 | 6.65 |
| CHEMBL5200637 | — | — | 1 | 6.61 |
| CHEMBL5204970 | — | — | 1 | 6.43 |
| CHEMBL5206436 | — | — | 1 | 6.42 |
| CHEMBL5200988 | — | — | 1 | 6.27 |
| CHEMBL5202129 | — | — | 1 | 6.10 |
| CHEMBL5207462 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196360 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5191510 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5201543 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5206902 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5177272 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5191674 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5182553 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5198812 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4443062 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5172573 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5207108 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5197154 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5177306 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5176460 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5208065 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5178865 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5173701 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5178571 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5195912 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5187605 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5178754 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4214567 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL5204270 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5200637 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL5204970 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL5206436 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5200988 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL5202129 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL5207462 | — | IC50 | = | 1670.0 | nM | 5.78 |