Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0005050 |
| PMID | 22112293 |
| Assay Used | - |
| Experimently Validated | Yes |
| EGFR (IC50) | 5nM |
| HER2 (IC50) | - |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | - |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | 91% |
| 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 | - |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | A431 human vulvar squamous carcinoma cells overexpressing HER-1 | 1000 nM | - | - | - | - | - | - | - | - | |||
| 2 | BGC-823 | - | 4060 nM | - | - | - | - | - | - | - | - | |||
| 3 | A549 | carcinomic human alveolar basal epithelial cell | 12160 nM | - | - | - | - | - | - | - | - | |||
| 4 | H460 | human NSCLC cells harboring wild-type EGFR | 16080 nM | - | - | - | - | - | - | - | - | |||
| 5 | HCT8 | - | 40710 nM | - | - | - | - | - | - | - | - | |||
| 6 | KB | - | > 200000 nM | - | - | - | - | - | - | - | - | |||
| 7 | Bel-7402 | - | > 200000 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | - |
| Mutant | L858R , L861Q , T790M , T790M/L858R |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |