| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001924 |
| PMID | 17827009 |
| Assay Used | The protein tyrosine Kinase activity was detrermined by measuring the initial velocity of turnover of peptide substrate pp60v-src & Cell-based EGFR Autophosphorylation (Y1068) of A431 |
| Experimently Validated | Yes |
| EGFR (IC50) | - |
| 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) | 220 nM |
| Ki (HER2) | - |
| Ki (HER4) | - |
| Kd (EGFR) | - |
| Kd (L858R) | - |
| Kd (T790M) | - |
| Kd (L858R/T790M) | - |
| Kd (Other mutation) | - |
| Note | The paper describes synthesis and structure–activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors |
| Extra | - |
| |
