|
|
|
|
|
|
|
|
|
|
Experimental Information | |
Enzymatic Activity | |
Molecule Id | EGIN0004885 |
PMID | 22169601 |
Assay Used | Kinase assay |
Experimently Validated | Yes |
EGFR (IC50) | - |
HER2 (IC50) | - |
HER4 (IC50) | - |
Mutant L858R (IC50) | - |
Mutant T790M (IC50) | - |
Double Mutant (IC50) | - |
Average ERBB2 and ERBB1 (IC50) | - |
Inhibition EGFR (%) | 68 ± 5 % |
Inhibitory Concentration | 1 µM |
Inhibition HER2 (%) | 24 ± 3 % |
Inhibitory Concentration | 1 µM |
Ki (EGFR) | - |
Ki (HER2) | - |
Ki (HER4) | - |
Kd (EGFR) | - |
Kd (L858R) | - |
Kd (T790M) | - |
Kd (L858R/T790M) | - |
Kd (Other mutation) | - |
Note | The paper describes the Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanone |
Extra | - |
Cellular Activity | ||||||||||||||
S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
Activity against Receptor | |
EGFR | Yes |
HER2 | Yes |
HER4 | - |
Wild type | Yes |
Mutant | - |
Inhibitor Binding | |
EGFR | - |
HER2 | - |
HER4 | - |