Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000005 |
| PMID | 20033049 |
| Assay Used | Kinase and Cellular assay |
| Experimently Validated | Yes |
| EGFR (IC50) | - |
| HER2 (IC50) | - |
| 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 Novel mutant-selective EGFR kinase inhibitors against EGFR T790M |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | Ba/F3 | ERBB2(WT) | 760 nM | - | - | - | - | - | - | - | - | |||
| 2 | Ba/F3 | EGFR(vIII) | 454 nM | - | - | - | - | - | - | - | - | |||
| 3 | Ba/F3 | EGFR(L858R) | 3 nM | - | - | - | - | - | - | - | - | |||
| 4 | Ba/F3 | EGFR(E746_A750) | 2 nM | - | - | - | - | - | - | - | - | |||
| 5 | Ba/F3 | ERBB2(Ins 774YVMA) | 2300 nM | - | - | - | - | - | - | - | - | |||
| 6 | Ba/F3 | ERBB2(Ins G776V, C) | 1900 nM | - | - | - | - | - | - | - | - | |||
| 7 | Ba/F3 | EGFR(L858R/T790M) | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 8 | Ba/F3 | EGFR(L858R/T790M/C797S) | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 9 | Ba/F3 | EGFR(E746_A750/T790M) | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 10 | Ba/F3 | EGFR(E746_A750/T790M/C797S) | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 11 | Ba/F3 | EGFR(A767_V769dupASV) | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 12 | CaLu3 | ERBB2 amp | 2700 nM | - | - | - | - | - | - | - | - | |||
| 13 | H1781 | ERBB2 Ins G776V, C | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 14 | H1819 | ERBB2 amp | 307 nM | - | - | - | - | - | - | - | - | |||
| 15 | H1975 | EGFR L858R/T790M | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 16 | H3255 | EGFR L858R | 22 nM | - | - | - | - | - | - | - | - | |||
| 17 | HCC827 | EGFR Del E746_A750 | 8 nM | - | - | - | - | - | - | - | - | |||
| 18 | HCC827 GR | EGFR E746_A750/MET amp | > 3300 nM | - | - | - | - | - | - | - | - | |||
| 19 | HN11 | EGFR & ERBB2 WT | 244 nM | - | - | - | - | - | - | - | - | |||
| 20 | PC9 | EGFR Del E746_A750 | 17 nM | - | - | - | - | - | - | - | - | |||
| 21 | PC9 GR | EGFR Del E746_A750/T790M | > 3300 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | EGFR-(Del E746_A750),EGFR-(L858R),EGFR-(L858R/T790M),EGFR-(Del E746_A750/T790M),EGFR-(E746_A750/MET),EGFR-(L858R/T790M/C797S),EGFR-(E746_A750/T790M/C797S),EGFR-(vIII),EGFR-(A767_V769dupASV),ERBB2-(Ins G776V, C),ERBB2-(Ins 774YVMA) |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |