Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0004525 |
| PMID | 21208802 |
| Assay Used | Cellular 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 (%) | - |
| 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 describesDiscovery of selective irreversible inhibitors for EGFR-T790M |
| Extra | >3300 nM(Ba/F3 cell-L858R/T790M/C797S),2nM(Ba/F3 cell-E746_A750_del/T790M),>3300 nM(Ba/F3 cell-E746_A750_del/T790M/C797S) |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | Ba/F3 | L858R/T790M | - | - | - | - | - | 8 nM | - | - | - | |||
| 2 | Ba/F3 | E746_A750_del/T790M | - | - | - | - | - | 2 nM | - | - | - | |||
| 3 | Ba/F3 | L858R/T790M/C797S | - | - | - | - | - | > 3300 nM | - | - | - | |||
| 4 | Ba/F3 | E746_A750_del/T790M/C797S | - | - | - | - | - | > 3300 nM | - | - | - | |||
| 5 | PC9 | EGFR-E746_A750_del | - | - | - | - | - | 36 nM | - | - | - | |||
| 6 | PC9 | E746_A750_del/T790M | - | - | - | - | - | 14 nM | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | - |
| Mutant | L858R/T790M,L858R/T790M/C797S,E746_A750_del/T790M/C797S |
| Inhibitor Binding | |
| EGFR | CYS797 |
| HER2 | - |
| HER4 | - |