Assay Detail
Binding
CHEMBL4394506
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Binding affinity to wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system by Kinomescan method
22
Total Activities
22
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
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 8.07 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 9.72 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.60 |
| CHEMBL1092250 | — | — | 1 | 9.57 |
| CHEMBL304929 | — | — | 1 | 9.26 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.15 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.00 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.96 |
| CHEMBL4467033 | — | — | 1 | 8.89 |
| CHEMBL4440586 | — | — | 1 | 8.74 |
| CHEMBL111038 | — | — | 1 | 8.62 |
| CHEMBL81073 | — | — | 1 | 8.13 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.02 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.96 |
| CHEMBL309682 | — | — | 1 | 7.66 |
| CHEMBL4447797 | — | — | 1 | 7.50 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.46 |
| CHEMBL4468521 | — | — | 1 | 7.28 |
| CHEMBL98248 | — | — | 1 | 7.24 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.66 |
| CHEMBL1089203 | — | — | 1 | 6.41 |
| CHEMBL311959 | — | — | 1 | 6.39 |
| CHEMBL4446630 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | Kd | = | 0.19 | nM | 9.72 |
| CHEMBL1173655 | AFATINIB | Kd | = | 0.25 | nM | 9.60 |
| CHEMBL1092250 | — | Kd | = | 0.27 | nM | 9.57 |
| CHEMBL304929 | — | Kd | = | 0.55 | nM | 9.26 |
| CHEMBL553 | ERLOTINIB | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL939 | GEFITINIB | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL180022 | NERATINIB | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4467033 | — | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL4440586 | — | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL111038 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL81073 | — | Kd | = | 7.4 | nM | 8.13 |
| CHEMBL24828 | VANDETANIB | Kd | = | 9.5 | nM | 8.02 |
| CHEMBL554 | LAPATINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL309682 | — | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL4447797 | — | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL4468521 | — | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL98248 | — | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL1089203 | — | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL311959 | — | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL4446630 | — | Kd | = | 6100.0 | nM | 5.21 |