| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0000005 |
| PMID | 0 |
| Assay Used | Alpha Screen P-Tyr-100 assay kit |
| Experimently Validated | Yes |
| EGFR (IC50) | 56 nM |
| HER2 (IC50) | - |
| 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 7,8-dihydro-[1,4]dioxino-[2,3-g]quinazolines as novel Epidermal Growth Factor Receptor Kinase Inhibitors |
| Extra | The compound 3e and 3f with 3-bromo aniline are much more potent than ZD-1839 |
| |
