Assay Detail
Binding
CHEMBL3223695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR kinase L858R/T790M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of new molecules inhibiting epidermal growth factor receptor threonine790 methionine790 mutant
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.50 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229592 | — | — | 1 | 8.74 |
| CHEMBL3219133 | — | — | 1 | 8.05 |
| CHEMBL3219347 | — | — | 1 | 7.85 |
| CHEMBL3219129 | — | — | 1 | 7.61 |
| CHEMBL3219348 | — | — | 1 | 7.48 |
| CHEMBL3219127 | — | — | 1 | 7.39 |
| CHEMBL3219128 | — | — | 1 | 7.29 |
| CHEMBL3219125 | — | — | 1 | 7.28 |
| CHEMBL3219134 | — | — | 1 | 7.27 |
| CHEMBL3219135 | — | — | 1 | 7.23 |
| CHEMBL3219130 | — | — | 1 | 7.06 |
| CHEMBL3219132 | — | — | 1 | 6.71 |
| CHEMBL3219126 | — | — | 1 | - |
| CHEMBL3219131 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229592 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL3219133 | — | IC50 | = | 8.95 | nM | 8.05 |
| CHEMBL3219347 | — | IC50 | = | 14.08 | nM | 7.85 |
| CHEMBL3219129 | — | IC50 | = | 24.83 | nM | 7.61 |
| CHEMBL3219348 | — | IC50 | = | 32.83 | nM | 7.48 |
| CHEMBL3219127 | — | IC50 | = | 40.73 | nM | 7.39 |
| CHEMBL3219128 | — | IC50 | = | 50.85 | nM | 7.29 |
| CHEMBL3219125 | — | IC50 | = | 52.63 | nM | 7.28 |
| CHEMBL3219134 | — | IC50 | = | 53.94 | nM | 7.27 |
| CHEMBL3219135 | — | IC50 | = | 59.36 | nM | 7.23 |
| CHEMBL3219130 | — | IC50 | = | 87.45 | nM | 7.06 |
| CHEMBL3219132 | — | IC50 | = | 193.97 | nM | 6.71 |
| CHEMBL3219126 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219131 | — | IC50 | > | 1000.0 | nM | - |