Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000003 |
| PMID | 18287036 |
| Assay Used | Enzyme and Cellular assays |
| Experimently Validated | Yes |
| EGFR (IC50) | 11 nM |
| HER2 (IC50) | 9 nM |
| HER4 (IC50) | 367 nM |
| 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-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | BT474 | - | 100 nM | - | - | - | - | - | - | - | - | |||
| 2 | HFF | - | 12000 nM | - | - | - | - | - | - | - | - | |||
| 3 | HN5 | - | 120 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | Yes |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |