| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0000220 |
| PMID | 10753475 |
| Assay Used | Inhibition of phos-phorylation of a random glutamic acid/tyrosine copolymer substrate by isolated EGFR enzyme, inhibition of EGF-stimulated Autophosphorylation of EGFR in A431 cells |
| Experimently Validated | Yes |
| EGFR (IC50) | 1.8 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 ppaer describes the Irreversible Inhibitors of the Epidermal Growth Factor Receptor 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides. |
| Extra | Isolated enzyme IC50 Values are the averages from at least two independent dose response curves; variation was generally 15% |
| |
