Assay Detail
Binding
CHEMBL3375801
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type EGFR (unknown origin) by high-throughput biochemical screening
12
Total Activities
12
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 | 12 | 6.54 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 10.00 |
| CHEMBL3354183 | — | — | 1 | 7.00 |
| CHEMBL3354191 | — | — | 1 | 6.50 |
| CHEMBL3354189 | — | — | 1 | 6.26 |
| CHEMBL3354190 | — | — | 1 | 6.25 |
| CHEMBL3354192 | — | — | 1 | 6.21 |
| CHEMBL3354184 | — | — | 1 | 6.14 |
| CHEMBL3352835 | — | — | 1 | 6.13 |
| CHEMBL3354188 | — | — | 1 | 5.96 |
| CHEMBL3354195 | — | — | 1 | 5.82 |
| CHEMBL3354193 | — | — | 1 | 5.72 |
| CHEMBL3354194 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3354183 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL3354191 | — | Ki | = | 317.0 | nM | 6.50 |
| CHEMBL3354189 | — | Ki | = | 553.0 | nM | 6.26 |
| CHEMBL3354190 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL3354192 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL3354184 | — | Ki | = | 716.0 | nM | 6.14 |
| CHEMBL3352835 | — | Ki | = | 743.0 | nM | 6.13 |
| CHEMBL3354188 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3354195 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3354193 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL3354194 | — | Ki | > | 2500.0 | nM | - |