Assay Detail
Binding
CHEMBL3860367
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 6x-HIS-tagged human recombinant EGFR (696 to 1022 residues) L858R/T790M mutant expressed in Sf9 cells pre-incubated for 90 mins followed by 1 mM ATP addition by HTRF assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3953221 | — | — | 1 | 8.40 |
| CHEMBL3959632 | — | — | 1 | 8.40 |
| CHEMBL3961202 | — | — | 1 | 8.00 |
| CHEMBL3953921 | — | — | 1 | 7.70 |
| CHEMBL3966111 | — | — | 1 | 7.30 |
| CHEMBL3973973 | — | — | 1 | 7.22 |
| CHEMBL3892960 | — | — | 1 | 5.17 |
| CHEMBL3982602 | — | — | 1 | 4.78 |
| CHEMBL3921545 | — | — | 1 | - |
| CHEMBL3894391 | — | — | 1 | - |
| CHEMBL3901943 | — | — | 1 | - |
| CHEMBL3972987 | — | — | 1 | - |
| CHEMBL3961970 | — | — | 1 | - |
| CHEMBL3981978 | — | — | 1 | - |
| CHEMBL3944524 | — | — | 1 | - |
| CHEMBL3962999 | — | — | 1 | - |
| CHEMBL3935558 | — | — | 1 | - |
| CHEMBL3936272 | — | — | 1 | - |
| CHEMBL3916436 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3953221 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3959632 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3961202 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3953921 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3966111 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3973973 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3892960 | — | IC50 | = | 6810.0 | nM | 5.17 |
| CHEMBL3982602 | — | IC50 | = | 16460.0 | nM | 4.78 |
| CHEMBL3921545 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3894391 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3901943 | — | IC50 | < | 2.0 | nM | - |
| CHEMBL3972987 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3961970 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3981978 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3944524 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3962999 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3935558 | — | IC50 | > | 32770.0 | nM | - |
| CHEMBL3936272 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3916436 | — | IC50 | > | 50000.0 | nM | - |