Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000376 |
| PMID | 15711537 |
| Assay Used | Kinase assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 1 nM |
| HER2 (IC50) | 77 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) | 0.44 nM |
| Kd (L858R) | 0.41 nM |
| Kd (T790M) | - |
| Kd (L858R/T790M) | - |
| Kd (Other mutation) | 0.27 nM( L747-S752del P753S),0.24 nM( L747-E749del A750P),0.23 nM( L747-T751del insS),0.44 nM( L861Q),0.24 nM( G719C),0.38 nM( E746-A750del),0.42 nM( G719S),0.33 nM( S752-I759del) |
| Note | The paper presents A small molecule kinase interaction map for clinical kinase inhibitors |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | L858R(Ka -value only) |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |