Epidermal Growth Factor Receptor Inhibitor Database
|
|
|
|
|
|
|
|
|
|
|
| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000005 |
| PMID | 18313807 |
| Assay Used | MTT 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 synthesis and cytotoxicity of 2,3-disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines against five human cancer cell lines (A549,K562,Molt-4,PC-3,MDA-MB-231) |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A549 | - | 13590 ± 2050 nM | - | - | - | - | - | - | - | - | |||
| 2 | K562 | - | 9360 ± 1130 nM | - | - | - | - | - | - | - | - | |||
| 3 | MDA-MB-231 | - | 36610 ±6080 nM | - | - | - | - | - | - | - | - | |||
| 4 | Molt-4 | - | 15020 ±320 nM | - | - | - | - | - | - | - | - | |||
| 5 | PC3 | - | 15100 ±3780 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |