Assay Detail
Binding
CHEMBL4011053
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using KHKKLAEGSAYEEV as substrate after 30 mins in presence of gamma-[32P]ATP by densitometry
53
Total Activities
53
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
First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 7.51 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097369 | — | — | 1 | 8.08 |
| CHEMBL4075530 | — | — | 1 | 8.05 |
| CHEMBL4103464 | — | — | 1 | 8.05 |
| CHEMBL4092951 | — | — | 1 | 8.04 |
| CHEMBL4075103 | — | — | 1 | 8.02 |
| CHEMBL4065288 | — | — | 1 | 7.99 |
| CHEMBL3815163 | — | — | 1 | 7.97 |
| CHEMBL4091921 | — | — | 1 | 7.94 |
| CHEMBL4102455 | — | — | 1 | 7.80 |
| CHEMBL4076434 | — | — | 1 | 7.80 |
| CHEMBL4088718 | — | — | 1 | 7.76 |
| CHEMBL4089588 | — | — | 1 | 7.71 |
| CHEMBL4097862 | — | — | 1 | 7.71 |
| CHEMBL4078182 | — | — | 1 | 7.69 |
| CHEMBL4101774 | — | — | 1 | 7.66 |
| CHEMBL4066504 | — | — | 1 | 7.60 |
| CHEMBL4062528 | — | — | 1 | 7.57 |
| CHEMBL4071170 | — | — | 1 | 7.55 |
| CHEMBL4088760 | — | — | 1 | 7.45 |
| CHEMBL4072769 | — | — | 1 | 7.43 |
| CHEMBL4067514 | — | — | 1 | 7.31 |
| CHEMBL4092966 | — | — | 1 | 7.26 |
| CHEMBL4085352 | — | — | 1 | 7.22 |
| CHEMBL4065300 | — | — | 1 | 7.22 |
| CHEMBL4080711 | — | — | 1 | 7.20 |
| CHEMBL4093114 | — | — | 1 | 6.95 |
| CHEMBL4072986 | — | — | 1 | 6.92 |
| CHEMBL4065503 | — | — | 1 | 6.92 |
| CHEMBL4077608 | — | — | 1 | 6.89 |
| CHEMBL4072928 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097369 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4075530 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4103464 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4092951 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4075103 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4065288 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL3815163 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4091921 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4102455 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4076434 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4088718 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL4089588 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL4097862 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4078182 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL4101774 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4066504 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL4062528 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL4071170 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL4088760 | — | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL4072769 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL4067514 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL4092966 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL4085352 | — | IC50 | = | 60.7 | nM | 7.22 |
| CHEMBL4065300 | — | IC50 | = | 60.1 | nM | 7.22 |
| CHEMBL4080711 | — | IC50 | = | 63.6 | nM | 7.20 |
| CHEMBL4093114 | — | IC50 | = | 112.4 | nM | 6.95 |
| CHEMBL4065503 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4072986 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4077608 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4072928 | — | IC50 | = | 133.1 | nM | 6.88 |
| CHEMBL4073912 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4077419 | — | IC50 | = | 146.3 | nM | 6.83 |
| CHEMBL4087010 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4063757 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4096625 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4079151 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4098758 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4070047 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4094706 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4061372 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4097454 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4099653 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4064174 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL4061460 | — | IC50 | - | — | - | |
| CHEMBL4071935 | — | IC50 | > | 150.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | = | 4.0 | nM | - |
| CHEMBL4070190 | — | IC50 | - | — | - | |
| CHEMBL3133904 | — | IC50 | = | 1.5 | nM | - |
| CHEMBL3132872 | — | IC50 | = | 2.1 | nM | - |
| CHEMBL4101828 | — | IC50 | > | 150.0 | nM | - |