Assay Detail
Functional
CHEMBL5160914
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC827 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.90 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185820 | — | — | 1 | 9.48 |
| CHEMBL5173237 | — | — | 1 | 9.42 |
| CHEMBL5202214 | — | — | 1 | 9.33 |
| CHEMBL2178352 | — | — | 1 | 9.03 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.00 |
| CHEMBL5184446 | — | — | 1 | 8.94 |
| CHEMBL5204635 | — | — | 1 | 8.80 |
| CHEMBL5208749 | — | — | 1 | 8.78 |
| CHEMBL5192520 | — | — | 1 | 8.78 |
| CHEMBL5178536 | — | — | 1 | 8.75 |
| CHEMBL5179946 | — | — | 1 | 8.74 |
| CHEMBL5188212 | — | — | 1 | 8.66 |
| CHEMBL5173023 | — | — | 1 | 8.61 |
| CHEMBL5179452 | — | — | 1 | 8.59 |
| CHEMBL5170905 | — | — | 1 | 8.52 |
| CHEMBL5194346 | — | — | 1 | 8.27 |
| CHEMBL5178388 | — | — | 1 | 8.05 |
| CHEMBL5192418 | — | — | 1 | 7.44 |
| CHEMBL5191971 | — | — | 1 | 7.22 |
| CHEMBL5184717 | — | — | 1 | 7.21 |
| CHEMBL5171149 | — | — | 1 | 7.17 |
| CHEMBL5198335 | — | — | 1 | 7.12 |
| CHEMBL5174906 | — | — | 1 | 7.07 |
| CHEMBL5207320 | — | — | 1 | 6.96 |
| CHEMBL5204884 | — | — | 1 | 6.89 |
| CHEMBL5199988 | — | — | 1 | 6.85 |
| CHEMBL5204201 | — | — | 1 | 6.82 |
| CHEMBL5202759 | — | — | 1 | 6.26 |
| CHEMBL5187191 | — | — | 1 | 6.17 |
| CHEMBL5182033 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185820 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5173237 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5202214 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2178352 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5184446 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL5204635 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5208749 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5192520 | — | IC50 | = | 1.66 | nM | 8.78 |
| CHEMBL5178536 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL5179946 | — | IC50 | = | 1.83 | nM | 8.74 |
| CHEMBL5188212 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL5173023 | — | IC50 | = | 2.48 | nM | 8.61 |
| CHEMBL5179452 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL5170905 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL5194346 | — | IC50 | = | 5.39 | nM | 8.27 |
| CHEMBL5178388 | — | IC50 | = | 8.93 | nM | 8.05 |
| CHEMBL5192418 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL5191971 | — | IC50 | = | 59.61 | nM | 7.22 |
| CHEMBL5184717 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5171149 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5198335 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5174906 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5207320 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5204884 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5199988 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5204201 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5202759 | — | IC50 | = | 544.0 | nM | 6.26 |
| CHEMBL5187191 | — | IC50 | = | 683.0 | nM | 6.17 |
| CHEMBL5182033 | — | IC50 | = | 768.0 | nM | 6.12 |
| CHEMBL5176927 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL5201463 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5181560 | — | IC50 | > | 10000.0 | nM | - |