Experimental Information |
|
Enzymatic Activity |
Molecule Id | EGIN0001609 |
PMID | 18287036 |
Assay Used | Enzyme and Cellular assays |
Experimently Validated | Yes |
EGFR (IC50) | 372 nM |
HER2 (IC50) | 52 nM |
HER4 (IC50) | 1349 nM |
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 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases |
Extra | 0,0(% Alkylation of EGFR in 3h and 20h) |
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