| + |
afatinib | down-regulates activity 
chemical inhibition
|
ErbB receptor family |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259443 |
|
|
Homo sapiens |
Non-small Cell Lung Cancer Cell |
| pmid |
sentence |
| 24643470 |
This manuscript comprehensively reviews the preclinical data on afatinib, an irreversible inhibitor of the tyrosine kinase activity of members of the epidermal growth factor receptor family (ErbB) including EGFR, HER2 and ErbB4. Afatinib covalently binds to cysteine 797 of the EGFR and the corresponding cysteines 805 and 803 in HER2 and ErbB4, respectively. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259440 |
|
|
Homo sapiens |
Lung Cancer Cell |
| pmid |
sentence |
| 22452896 |
Afatinib, an irreversible erbb-family blocker, has shown preclinical activity when tested in egfr mutant models with mutations that confer resistance to egfr tyrosine-kinase inhibitors. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259442 |
|
|
Homo sapiens |
Breast Cancer Cell |
| pmid |
sentence |
| 22418700 |
Afatinib is an oral, erbb family blocker, which covalently binds and irreversibly blocks all kinase-competent erbb family members. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259441 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here. |
|
| Publications: |
4 |
Organism: |
Homo Sapiens, In Vitro |
| + |
afatinib | down-regulates
chemical inhibition
|
EGFR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189356 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-196760 |
|
|
Homo sapiens |
Lung Cancer Cell |
| pmid |
sentence |
| 22452896 |
Afatinib, an irreversible erbb-family blocker, has shown preclinical activity when tested in egfr mutant models with mutations that confer resistance to egfr tyrosine-kinase inhibitors. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
afatinib | down-regulates
chemical inhibition
|
ERBB2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-196621 |
|
|
Homo sapiens |
Breast Cancer Cell |
| pmid |
sentence |
| 22418700 |
Afatinib is an oral, erbb family blocker, which covalently binds and irreversibly blocks all kinase-competent erbb family members. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189359 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
afatinib | down-regulates activity
chemical inhibition
|
ERBB2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258066 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
afatinib | down-regulates activity
chemical inhibition
|
EGFR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258169 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
afatinib | down-regulates activity
chemical inhibition
|
ERBB4 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259295 |
|
|
Homo sapiens |
Non-small Cell Lung Cancer Cell |
| pmid |
sentence |
| 24643470 |
This manuscript comprehensively reviews the preclinical data on afatinib, an irreversible inhibitor of the tyrosine kinase activity of members of the epidermal growth factor receptor family (ErbB) including EGFR, HER2 and ErbB4. Afatinib covalently binds to cysteine 797 of the EGFR and the corresponding cysteines 805 and 803 in HER2 and ErbB4, respectively. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
afatinib
