Assay Detail
Binding
CHEMBL5238849
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGR-induced EGFR phosphorylation in human A549 cells pretreated for 2 hrs followed by EGF stimulation by immune assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.20 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.46 |
| CHEMBL5270000 | — | — | 1 | 7.82 |
| CHEMBL5284387 | — | — | 1 | 7.82 |
| CHEMBL5291353 | — | — | 1 | 7.82 |
| CHEMBL5268143 | — | — | 1 | 7.72 |
| CHEMBL5284486 | — | — | 1 | 7.70 |
| CHEMBL5266834 | — | — | 1 | 7.64 |
| CHEMBL5281266 | — | — | 1 | 7.64 |
| CHEMBL5266798 | — | — | 1 | 7.62 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 7.51 |
| CHEMBL5275712 | — | — | 1 | 7.50 |
| CHEMBL5283216 | — | — | 1 | 7.46 |
| CHEMBL5284255 | — | — | 1 | 7.44 |
| CHEMBL5279794 | — | — | 1 | 7.41 |
| CHEMBL5286091 | — | — | 1 | 7.40 |
| CHEMBL5279491 | — | — | 1 | 7.38 |
| CHEMBL5290929 | — | — | 1 | 7.37 |
| CHEMBL5271640 | — | — | 1 | 7.35 |
| CHEMBL5271718 | — | — | 1 | 7.31 |
| CHEMBL5270335 | — | — | 1 | 7.24 |
| CHEMBL5266482 | — | — | 1 | 7.15 |
| CHEMBL5266100 | — | — | 1 | 7.10 |
| CHEMBL5273438 | — | — | 1 | 7.08 |
| CHEMBL3353404 | — | — | 1 | 7.02 |
| CHEMBL5272345 | — | — | 1 | 6.85 |
| CHEMBL5276760 | — | — | 1 | 6.83 |
| CHEMBL5291010 | — | — | 1 | 6.68 |
| CHEMBL5281203 | — | — | 1 | 6.65 |
| CHEMBL5266896 | — | — | 1 | 6.54 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5270000 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5291353 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5284387 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5268143 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5284486 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5266834 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5281266 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5266798 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5275712 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5283216 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5284255 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5279794 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5286091 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5279491 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5290929 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5271640 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5271718 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5270335 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5266482 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5266100 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5273438 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3353404 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5272345 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5276760 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5291010 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5281203 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL5266896 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4104658 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 1983.0 | nM | 5.70 |
| CHEMBL5286532 | — | IC50 | = | 2969.0 | nM | 5.53 |