Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0003339 |
| PMID | 15715478 |
| Assay Used | Kinase and Cellular inhibition assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 165 nM |
| HER2 (IC50) | 281 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 Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | - | 254 nM | - | - | - | - | - | - | - | - | |||
| 2 | SKBR3 | - | 31.9 nM | - | - | - | - | - | - | - | - | |||
| 3 | SW620 | - | 500 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | Cys773 |
| HER2 | CYS805 |
| HER4 | - |