Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0005100 |
| PMID | 23116168 |
| Assay Used | Kinase Inhibition assay using KinaseProfiler |
| Experimently Validated | Yes |
| EGFR (IC50) | 4 nM |
| HER2 (IC50) | 60 nM |
| HER4 (IC50) | 30 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) | 0.0006 然 |
| Kd (L858R) | 0.0006 然 |
| Kd (T790M) | - |
| Kd (L858R/T790M) | 0.0016 然 |
| Kd (Other mutation) | (G719C):0.0007 然,(G719S):0.0005 然,(L861Q):0.0007 然 |
| Note | - |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | HCC827 | cell line harbors EGFR-activating mutation (deletion mutation) | < 0.01 nM | - | - | - | - | - | - | - | - | |||
| 2 | H1975 | cell line bears the drug resistance mutation in EGFR (L858R/T790M) | 360 nM | - | - | - | - | - | - | - | - | |||
| 3 | HepG2 | human hepatocellular carcinoma cell line | > 5000 nM | - | - | - | - | - | - | - | - | |||
| 4 | PC9 | NSCLC Del E746_A750(EGFR mutant) | 0.22 nM | - | - | - | - | - | - | - | - | |||
| 5 | Calu3 | NSCLC ErbB2overexpressed | 120 nM | - | - | - | - | - | - | - | - | |||
| 6 | H292 | NSCLC EGFRoverexpressed | 45 nM | - | - | - | - | - | - | - | - | |||
| 7 | A431 | epidermal EGFRoverexpressed | 120 nM | - | - | - | - | - | - | - | - | |||
| 8 | Fadu | hypopharyngeal EGFRoverexpressed | 15 nM | - | - | - | - | - | - | - | - | |||
| 9 | MDA-MB-231 | breast KRAS mutation(G13D) | 5000 nM | - | - | - | - | - | - | - | - | |||
| 10 | HCT116 | colon KRAS and PI3kmutations | 3000 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | Yes |
| Wild type | Yes |
| Mutant | Yes |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |