| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001964 |
| PMID | 17869514 |
| Assay Used | EGFR Kinase assays ,cellular erbB2 Autophosphorylation assay and Antipliferative assay. |
| Experimently Validated | Yes |
| EGFR (IC50) | 97 ± 64 nM |
| HER2 (IC50) | < 2 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 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of the erbB2 |
| Extra | 147 ± 79nM (Clone 24) |
| |
