| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0000010 |
| PMID | 8691423 |
| Assay Used | Inhibition of the tyrosine Kinase activity of a recombinant intracellular domain of the EGF-R (EGF-R ICD) ,using angiotensin II as the phosphate-acceptor substrate, Cellular assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 4 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 4-(Phenylamino)pyrrolopyrimidines as potent and selective, ATP Site Directed Inhibitors of the EGF-Receptor Protein Tyrosine Kinase. |
| Extra | - |
| |
