Assay Detail
Binding
CHEMBL4730561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant EGFR expressed in baculovirus infected Sf9 insect cells using poly (Glu, Tyr) 4:1 peptide as substrate incubated for 40 mins in presence of 10 uM ATP by ADP-Glo luminescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.75 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.66 |
| CHEMBL4743220 | — | — | 1 | 8.60 |
| CHEMBL4744655 | — | — | 1 | 8.41 |
| CHEMBL4783428 | — | — | 1 | 8.21 |
| CHEMBL4740063 | — | — | 1 | 8.19 |
| CHEMBL4791756 | — | — | 1 | 8.12 |
| CHEMBL4786961 | — | — | 1 | 8.00 |
| CHEMBL4759031 | — | — | 1 | 7.98 |
| CHEMBL1198370 | — | — | 1 | 7.87 |
| CHEMBL4793453 | — | — | 1 | 7.81 |
| CHEMBL4762453 | — | — | 1 | 7.79 |
| CHEMBL4749501 | — | — | 1 | 7.72 |
| CHEMBL4750375 | — | — | 1 | 7.71 |
| CHEMBL4794223 | — | — | 1 | 7.68 |
| CHEMBL4743464 | — | — | 1 | 7.66 |
| CHEMBL4778159 | — | — | 1 | 7.62 |
| CHEMBL4744207 | — | — | 1 | 7.60 |
| CHEMBL4759650 | — | — | 1 | 7.38 |
| CHEMBL4453068 | — | — | 1 | 7.31 |
| CHEMBL4786797 | — | — | 1 | 6.30 |
| CHEMBL4793944 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 2.17 | nM | 8.66 |
| CHEMBL4743220 | — | IC50 | = | 2.49 | nM | 8.60 |
| CHEMBL4744655 | — | IC50 | = | 3.91 | nM | 8.41 |
| CHEMBL4783428 | — | IC50 | = | 6.16 | nM | 8.21 |
| CHEMBL4740063 | — | IC50 | = | 6.41 | nM | 8.19 |
| CHEMBL4791756 | — | IC50 | = | 7.63 | nM | 8.12 |
| CHEMBL4786961 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4759031 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL1198370 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4793453 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL4762453 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4749501 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4750375 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL4794223 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4743464 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4778159 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4744207 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4759650 | — | IC50 | = | 41.4 | nM | 7.38 |
| CHEMBL4453068 | — | IC50 | = | 48.7 | nM | 7.31 |
| CHEMBL4786797 | — | IC50 | = | 505.1 | nM | 6.30 |
| CHEMBL4793944 | — | IC50 | = | 782.8 | nM | 6.11 |