Epidermal Growth Factor Receptor Inhibitor Database
|
|
|
|
|
|
|
|
|
|
|
| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000208 |
| PMID | 22280453 |
| Assay Used | Kinase and Cellular assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 1.69±1.6 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 Irreversible Inhibition of Epidermal Growth Factor Receptor Activity by 3-Aminopropanamides |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | H1975 | T790M | 160 ± 50 nM | - | - | - | - | - | - | 98±1.8 , 86±0.4 | percent Inhibtion at 1 µM(A549 at 1h) , percent Inhibtion at 1 µM(A549 at 8h after removal) | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | - |
| Mutant | T790M |
| Inhibitor Binding | |
| EGFR | CYS797 |
| HER2 | - |
| HER4 | - |