Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000003 |
| PMID | 21732342 |
| Assay Used | Kinase and Cellular assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 52.2 nM |
| HER2 (IC50) | 36.3 nM |
| HER4 (IC50) | > 1000 nM |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | > 1000 nM |
| Double Mutant (IC50) | > 1000 nM |
| 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 antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | EGFR (WT amplified) | - | - | - | 104.2 nM | - | - | - | - | - | |||
| 2 | A549 | K-ras mutation (G12S) | - | - | - | > 10000 nM | - | - | - | - | - | |||
| 3 | Balb/c3T3 | Mouse fibroblast | - | - | - | > 10000 nM | - | - | - | - | - | |||
| 4 | BT474 | HER-2 (WT amplified) | - | - | - | 30.6 nM | - | - | - | - | - | |||
| 5 | CaLu3 | HER-2 (WT amplified) | - | - | - | 27.8 nM | - | - | - | - | - | |||
| 6 | HCC827 | EGFR (Del E746_A750) | - | - | - | 271.4 nM | - | - | - | - | - | |||
| 7 | HS27 | Human fibroblast | - | - | - | > 10000 nM | - | - | - | - | - | |||
| 8 | MDA175 | HER-2 (WT) | - | - | - | 852 nM | - | - | - | - | - | |||
| 9 | NCI-H1781 | HER-2 (G776V Cins) | - | - | - | 3402 nM | - | - | - | - | - | |||
| 10 | NCI-H1975 | EGFR (L858R T790M) | - | - | - | > 1000 nM | - | - | - | - | - | |||
| 11 | NCI-H358 | EGFR (WT) | - | - | - | 420.7 nM | - | - | - | - | - | |||
| 12 | NCI-N87 | HER-2 (WT amplified) | - | - | - | 30.8 nM | - | - | - | - | - | |||
| 13 | SKBR3 | HER-2 (WT amplified) | - | - | - | 28.8 nM | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | Yes |
| Wild type | Yes |
| Mutant | T790M, T790M/L858R |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |