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Experimental Information | |
Enzymatic Activity | |
Molecule Id | EGIN0003357 |
PMID | 15715478 |
Assay Used | Kinase and Cellular inhibition assay |
Experimently Validated | Yes |
EGFR (IC50) | 15 nM |
HER2 (IC50) | 18 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 | - | 569 nM | - | - | - | - | - | - | - | - | |||
2 | SKBR3 | - | 28 nM | - | - | - | - | - | - | - | - | |||
3 | SW620 | - | 775 nM | - | - | - | - | - | - | - | - | |||
Activity against Receptor | |
EGFR | Yes |
HER2 | Yes |
HER4 | - |
Wild type | Yes |
Mutant | - |
Inhibitor Binding | |
EGFR | Cys773 |
HER2 | CYS805 |
HER4 | - |