Assay Detail
Functional
CHEMBL5160913
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| 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 | 35 | 6.50 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185820 | — | — | 1 | 7.92 |
| CHEMBL5202214 | — | — | 1 | 7.82 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.77 |
| CHEMBL5204635 | — | — | 1 | 7.50 |
| CHEMBL5179452 | — | — | 1 | 7.41 |
| CHEMBL5208749 | — | — | 1 | 7.40 |
| CHEMBL5179946 | — | — | 1 | 7.39 |
| CHEMBL5173237 | — | — | 1 | 7.39 |
| CHEMBL5192520 | — | — | 1 | 7.36 |
| CHEMBL5178388 | — | — | 1 | 6.90 |
| CHEMBL5192418 | — | — | 1 | 6.60 |
| CHEMBL5178536 | — | — | 1 | 6.58 |
| CHEMBL5191971 | — | — | 1 | 6.55 |
| CHEMBL5184446 | — | — | 1 | 6.54 |
| CHEMBL5170905 | — | — | 1 | 6.54 |
| CHEMBL2178352 | — | — | 1 | 6.47 |
| CHEMBL5188212 | — | — | 1 | 6.44 |
| CHEMBL5174578 | — | — | 1 | 6.26 |
| CHEMBL5171149 | — | — | 1 | 6.19 |
| CHEMBL5174906 | — | — | 1 | 6.15 |
| CHEMBL5207320 | — | — | 1 | 6.14 |
| CHEMBL5198335 | — | — | 1 | 6.12 |
| CHEMBL5187191 | — | — | 1 | 6.10 |
| CHEMBL5184717 | — | — | 1 | 6.01 |
| CHEMBL5171926 | — | — | 1 | 5.97 |
| CHEMBL5173023 | — | — | 1 | 5.93 |
| CHEMBL5199988 | — | — | 1 | 5.83 |
| CHEMBL5204884 | — | — | 1 | 5.77 |
| CHEMBL5202759 | — | — | 1 | 5.63 |
| CHEMBL5182033 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185820 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5202214 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5204635 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5179452 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5208749 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5179946 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5173237 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5192520 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5178388 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5192418 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5178536 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL5191971 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL5184446 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5170905 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2178352 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL5188212 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5174578 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5171149 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5174906 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL5207320 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5198335 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5187191 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5184717 | — | IC50 | = | 985.0 | nM | 6.01 |
| CHEMBL5171926 | — | IC50 | = | 1064.0 | nM | 5.97 |
| CHEMBL5173023 | — | IC50 | = | 1173.0 | nM | 5.93 |
| CHEMBL5199988 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL5204884 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5202759 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL5182033 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL5204201 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL5194346 | — | IC50 | = | 2901.0 | nM | 5.54 |
| CHEMBL5176927 | — | IC50 | = | 5794.0 | nM | 5.24 |
| CHEMBL5181560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5201463 | — | IC50 | > | 10000.0 | nM | - |