| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0001252 |
| PMID | 7902440 |
| Assay Used | Enzyme and cell assays |
| Experimently Validated | Yes |
| EGFR (IC50) | > 83000 nM |
| HER2 (IC50) | 15000 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 cis-benzylidenemalononitrile tyrphostins as inhibitors of ErbB family. |
| Extra | 4.4µM (EGFR-PolyGAT phosphorylation) |
| |
| Molecule Id | EGIN0001252 |
| PMID | 7902440 |
| Assay Used | Enzyme and cell assays |
| Experimently Validated | Yes |
| EGFR (IC50) | 19000 nM |
| HER2 (IC50) | 350 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 cis-benzylidenemalononitrile tyrphostins as inhibitors of ErbB family. |
| Extra | 18.6µM (EGFR-PolyGAT phosphorylation) |
| |
