| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001411 |
| PMID | 19208477 |
| Assay Used | Enzyme assay and Cell proliferation assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 1650 nM |
| HER2 (IC50) | 220 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 alkynyl thienopyrimidine as dual EGFR/ErbB-2 kinase inhibitors |
| Extra | 48% (%covalent modification of EGFR after 3 h) |
| |
