Assay Detail
Binding
CHEMBL4416105
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human EGFR kinase domain (696 to 1022 residues) using poly(Glu, Tyr) 4:1 substrate incubated for 60 mins by kinase-Glo plus luminescent kinase assay
26
Total Activities
26
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 a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.96 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4458437 | — | — | 1 | 7.89 |
| CHEMBL4463012 | — | — | 1 | 7.85 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.85 |
| CHEMBL4521381 | — | — | 1 | 7.82 |
| CHEMBL4583178 | — | — | 1 | 7.72 |
| CHEMBL1172843 | — | — | 1 | 7.70 |
| CHEMBL4559807 | — | — | 1 | 7.62 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.54 |
| CHEMBL4448691 | — | — | 1 | 7.21 |
| CHEMBL4456359 | — | — | 1 | 7.19 |
| CHEMBL4446953 | — | — | 1 | 7.10 |
| CHEMBL4556670 | — | — | 1 | 7.09 |
| CHEMBL4475546 | — | — | 1 | 7.09 |
| CHEMBL4447962 | — | — | 1 | 6.97 |
| CHEMBL4514452 | — | — | 1 | 6.93 |
| CHEMBL4534719 | — | — | 1 | 6.87 |
| CHEMBL4441440 | — | — | 1 | 6.80 |
| CHEMBL1172781 | — | — | 1 | 6.65 |
| CHEMBL4448148 | — | — | 1 | 6.62 |
| CHEMBL2310642 | — | — | 1 | 6.62 |
| CHEMBL4447289 | — | — | 1 | 6.38 |
| CHEMBL4450843 | — | — | 1 | 6.25 |
| CHEMBL4565374 | — | — | 1 | 5.51 |
| CHEMBL4447036 | — | — | 1 | 5.43 |
| CHEMBL4527132 | — | — | 1 | 5.30 |
| CHEMBL4531827 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4458437 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4463012 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4521381 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4583178 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1172843 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4559807 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL939 | GEFITINIB | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4448691 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4456359 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4446953 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4556670 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4475546 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4447962 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4514452 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4534719 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4441440 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL1172781 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4448148 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL2310642 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4447289 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL4450843 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL4565374 | — | IC50 | = | 3059.0 | nM | 5.51 |
| CHEMBL4447036 | — | IC50 | = | 3675.0 | nM | 5.43 |
| CHEMBL4527132 | — | IC50 | = | 5004.0 | nM | 5.30 |
| CHEMBL4531827 | — | IC50 | > | 10000.0 | nM | - |