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Experimental Information | |
Enzymatic Activity | |
Molecule Id | EGIN0004544 |
PMID | 22339342 |
Assay Used | FRET-based Z'-Lyte assay and MTT assay |
Experimently Validated | Yes |
EGFR (IC50) | 1.67 nM |
HER2 (IC50) | - |
HER4 (IC50) | - |
Mutant L858R (IC50) | 2.42 nM |
Mutant T790M (IC50) | 2.43 nM |
Double Mutant (IC50) | 6.31 nM |
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 Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 ? Methionine790 Mutant |
Extra | 2.56nM(EGFR-L861Q) |
Cellular Activity | ||||||||||||||
S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
1 | A431 | WT- overexpression | 1150 ± 60 nM | - | - | - | - | - | - | - | - | |||
2 | A549 | WT, k-Ras mutation | 2470 ± 600 nM | - | - | - | - | - | - | - | - | |||
3 | H1975 | L858R/T790M | 33 ± 11 nM | - | - | - | - | - | - | - | - | |||
4 | HCC827 | Del E746_A772 | 23 ± 1 nM | - | - | - | - | - | - | - | - | |||
5 | HL7702 | - | 2790 ± 1350 nM | - | - | - | - | - | - | - | - | |||
Activity against Receptor | |
EGFR | Yes |
HER2 | - |
HER4 | - |
Wild type | Yes |
Mutant | T790M,L858R,L861Q,L858R/T790M,Del E746_A750 |
Inhibitor Binding | |
EGFR | CYS797 |
HER2 | - |
HER4 | - |