Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000383 |
| PMID | 12502359 |
| Assay Used | Cytoplasmic domain is used and Autophosphorylation of these domains is studied so the values may differ from other studies. |
| Experimently Validated | Yes |
| EGFR (IC50) | 130 nM |
| HER2 (IC50) | 370 nM |
| 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 describes the 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitrilesas Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2). |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | - | 240 nM | - | - | - | - | - | - | - | - | |||
| 2 | SKBR3 | - | 80 nM | - | - | - | - | - | - | - | - | |||
| 3 | SW620 | - | 400 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | CYS773 |
| HER2 | CYS805 |
| HER4 | - |