Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0005142 |
| PMID | 24124898 |
| Assay Used | kinase activity assays were performed using the FRET-based Z?-Lyte assay |
| Experimently Validated | Yes |
| EGFR (IC50) | - |
| HER2 (IC50) | - |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | 9.2 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 | - |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | H1975 | gefitinib-resistant human lung cancer cell line (EGFRL858R/T790M). | 47 ± 12 nM | - | - | - | - | - | - | - | - | |||
| 2 | H460 | human NSCLC cells harboring wild-type EGFR | 16000 ± 8900 nM | - | - | - | - | - | - | - | - | |||
| 3 | 95D | human NSCLC cells harboring wild-type EGFR | 4000 ± 2400 nM | - | - | - | - | - | - | - | - | |||
| 4 | H1299 | human NSCLC cells harboring wild-type EGFR | 5100 ± 3400 nM | - | - | - | - | - | - | - | - | |||
| 5 | H358 | human NSCLC cells harboring wild-type EGFR | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 6 | HL7702 | diploid human liver cell line. | > 10000 nM | - | - | - | - | - | - | - | - | |||
| 7 | HCC827 | human NSCLC cell line with EGFR(del E746‑A750) | 5 ± 2 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | - |
| HER2 | - |
| HER4 | - |
| Wild type | - |
| Mutant | L858R/T790M |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |