| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0000003 |
| PMID | 22595177 |
| Assay Used | Homogeneous time-resolved fluorescence (HTRF) KinEASE-TK assay and MTT assay |
| Experimently Validated | yes |
| EGFR (IC50) | 9 ± 0.5 nM |
| HER2 (IC50) | - |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | - |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | 100 %, 99.9 % |
| Inhibitory Concentration | 100 µM , 10 µM |
| 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 decribed the discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening |
| Extra | - |
| |
