Assay Detail
Binding
CHEMBL3223693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR kinase L858R 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 | 7.64 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3219127 | — | — | 1 | 8.37 |
| CHEMBL1229592 | — | — | 1 | 8.09 |
| CHEMBL3219133 | — | — | 1 | 8.08 |
| CHEMBL3219348 | — | — | 1 | 8.04 |
| CHEMBL3219130 | — | — | 1 | 7.88 |
| CHEMBL3219125 | — | — | 1 | 7.82 |
| CHEMBL3219347 | — | — | 1 | 7.61 |
| CHEMBL3219132 | — | — | 1 | 7.51 |
| CHEMBL3219128 | — | — | 1 | 7.38 |
| CHEMBL3219134 | — | — | 1 | 7.30 |
| CHEMBL3219129 | — | — | 1 | 7.25 |
| CHEMBL3219135 | — | — | 1 | 7.21 |
| CHEMBL3219131 | — | — | 1 | 6.76 |
| CHEMBL3219126 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3219127 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1229592 | — | IC50 | = | 8.13 | nM | 8.09 |
| CHEMBL3219133 | — | IC50 | = | 8.33 | nM | 8.08 |
| CHEMBL3219348 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL3219130 | — | IC50 | = | 13.25 | nM | 7.88 |
| CHEMBL3219125 | — | IC50 | = | 15.11 | nM | 7.82 |
| CHEMBL3219347 | — | IC50 | = | 24.53 | nM | 7.61 |
| CHEMBL3219132 | — | IC50 | = | 30.74 | nM | 7.51 |
| CHEMBL3219128 | — | IC50 | = | 41.59 | nM | 7.38 |
| CHEMBL3219134 | — | IC50 | = | 50.02 | nM | 7.30 |
| CHEMBL3219129 | — | IC50 | = | 56.49 | nM | 7.25 |
| CHEMBL3219135 | — | IC50 | = | 62.19 | nM | 7.21 |
| CHEMBL3219131 | — | IC50 | = | 173.73 | nM | 6.76 |
| CHEMBL3219126 | — | IC50 | > | 1000.0 | nM | - |