Assay Detail
Binding
CHEMBL3375799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M/L858R mutant (unknown origin) by high-throughput biochemical screening
15
Total Activities
15
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
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.59 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 10.00 |
| CHEMBL3354191 | — | — | 1 | 7.92 |
| CHEMBL3352835 | — | — | 1 | 7.85 |
| CHEMBL3354187 | — | — | 1 | 7.80 |
| CHEMBL3354189 | — | — | 1 | 7.77 |
| CHEMBL3354192 | — | — | 1 | 7.75 |
| CHEMBL3354183 | — | — | 1 | 7.66 |
| CHEMBL3354184 | — | — | 1 | 7.55 |
| CHEMBL3354188 | — | — | 1 | 7.48 |
| CHEMBL3354190 | — | — | 1 | 7.40 |
| CHEMBL3354186 | — | — | 1 | 7.18 |
| CHEMBL3354185 | — | — | 1 | 7.12 |
| CHEMBL3354195 | — | — | 1 | 7.09 |
| CHEMBL3354193 | — | — | 1 | 6.94 |
| CHEMBL3354194 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3354191 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3352835 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3354187 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3354189 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3354192 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3354183 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3354184 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3354188 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3354190 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3354186 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL3354185 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL3354195 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL3354193 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL3354194 | — | Ki | = | 423.0 | nM | 6.37 |