Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0004548 |
| PMID | 22339342 |
| Assay Used | FRET-based Z'-Lyte assay and MTT assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 0.29 nM |
| HER2 (IC50) | - |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | 0.38 nM |
| Mutant T790M (IC50) | 0.67 nM |
| Double Mutant (IC50) | 0.93 nM |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | - |
| Inhibitory Concentration | - |
| Inhibition HER2 (%) | - |
| Inhibitory Concentration | - |
| Ki (EGFR) | - |
| Ki (HER2) | - |
| Ki (HER4) | - |
| Kd (EGFR) | 1.2 nM |
| Kd (L858R) | 1.3 nM |
| Kd (T790M) | 0.29 nM |
| Kd (L858R/T790M) | 0.30 nM |
| Kd (Other mutation) | 0.68 nM(EGFR-L861Q) |
| Note | The paper describes the Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 ? Methionine790 Mutant |
| Extra | 0.72nM(EGFR-L861Q) |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | WT- overexpression | 170 ± 30 nM | - | - | - | - | - | - | - | - | |||
| 2 | A549 | WT, k-Ras mutation | 2660 ± 330 nM | - | - | - | - | - | - | - | - | |||
| 3 | H1975 | L858R/T790M | 14 ± 6 nM | - | - | - | - | - | - | - | - | |||
| 4 | HCC827 | Del E746_A769 | 3 ± 1 nM | - | - | - | - | - | - | - | - | |||
| 5 | HL7702 | - | 2390 ± 530 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | Yes |
| Mutant | T790M,L858R,L861Q,L858R/T790M,Del E746_A750 |
| Inhibitor Binding | |
| EGFR | CYS797 |
| HER2 | - |
| HER4 | - |