Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0001093 |
| PMID | 17575237 |
| Assay Used | Enzymatic and in Cellular assays |
| Experimently Validated | Yes |
| EGFR (IC50) | 0.3 ± 0.1 nM |
| HER2 (IC50) | 16 ± 3 nM |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | 5 nM |
| 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 Inhibition of the T790M Gatekeeper Mutant of the Epidermal Growth Factor Receptor by EXEL-7647 |
| Extra | 13 nM/L(A431) |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | WT | 1 nM | - | - | - | - | - | - | - | - | |||
| 2 | H1975 | - | 0.92 nM | - | - | - | - | - | - | - | - | |||
| 3 | pCMV/Lx-1 | WT | 12 nM | - | - | - | - | - | - | - | - | |||
| 4 | pCMV/Lx-1 | L861Q | 10 nM | - | - | - | - | - | - | - | - | |||
| 5 | pTet-On/Lx-1 | WT | 5 nM | - | - | - | - | - | - | - | - | |||
| 6 | pTet-On/Lx-1 | Variant III | 74 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | L858R , L858R/T790M |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |