| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001627 |
| PMID | 18842405 |
| Assay Used | Enzyme and cell assays |
| Experimently Validated | Yes |
| EGFR (IC50) | 60 nM |
| HER2 (IC50) | 78 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 novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines based dual EGFR/ErbB-2 inhibitors. |
| Extra | 41% (% covalent modification of EGFR after 3 h.) |
| |
