| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001443 |
| PMID | 19111461 |
| Assay Used | Enzyme inhibition and cell proliferation ( MEB proliferation assay) |
| Experimently Validated | Yes |
| EGFR (IC50) | 68 nM |
| HER2 (IC50) | 246 nM |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | - |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | - |
| Inhibitory Concentration | - |
| Inhibition HER2 (%) | - |
| Inhibitory Concentration | - |
| Ki (EGFR) | - |
| Ki (HER2) | - |
| Ki (HER4) | - |
| Kd (EGFR) | - |
| Kd (L858R) | - |
| Kd (T790M) | - |
| Kd (L858R/T790M) | - |
| Kd (Other mutation) | - |
| Note | The paper describes the Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors |
| Extra | 0,15(% Alkylation of EGFR in 3h and 20h) |
| |
