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Experimental Information | |
Enzymatic Activity | |
Molecule Id | EGIN0004853 |
PMID | 22280453 |
Assay Used | Kinase and Cellular assay |
Experimently Validated | Yes |
EGFR (IC50) | 0.28±0.07 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 | 3690 ± 1100 nM | - | - | - | - | - | - | 97±1.4 , 89±1 | 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 | - |