| + |
dabrafenib | down-regulates activity 
chemical inhibition
|
RAF1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259218 |
|
|
in vitro |
|
| pmid |
sentence |
| 24720932 |
Dabrafenib is known to inhibit V600E, V600K and V600D BRAF enzymes with in vitro IC50 values of 0.65, 0.5 and 1.84 nM, respectively. Dabrafenib can inhibit wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. Other kinases (SIK1, NEK111 and LIMK1) can be inhibited by dabrafenib when administered in high concentrations |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
BRAF |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259215 |
|
|
in vitro |
|
| pmid |
sentence |
| 24720932 |
Dabrafenib is known to inhibit V600E, V600K and V600D BRAF enzymes with in vitro IC50 values of 0.65, 0.5 and 1.84 nM, respectively. Dabrafenib can inhibit wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. Other kinases (SIK1, NEK111 and LIMK1) can be inhibited by dabrafenib when administered in high concentrations |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
LIMK1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259216 |
|
|
in vitro |
|
| pmid |
sentence |
| 24720932 |
Dabrafenib is known to inhibit V600E, V600K and V600D BRAF enzymes with in vitro IC50 values of 0.65, 0.5 and 1.84 nM, respectively. Dabrafenib can inhibit wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. Other kinases (SIK1, NEK111 and LIMK1) can be inhibited by dabrafenib when administered in high concentrations |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
SIK1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259219 |
|
|
in vitro |
|
| pmid |
sentence |
| 24720932 |
Dabrafenib is known to inhibit V600E, V600K and V600D BRAF enzymes with in vitro IC50 values of 0.65, 0.5 and 1.84 nM, respectively. Dabrafenib can inhibit wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. Other kinases (SIK1, NEK111 and LIMK1) can be inhibited by dabrafenib when administered in high concentrations |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
CDK16 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261073 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 29112787 |
We have identified dabrafenib as a potent inhibitor of NEK9 and CDK16, and our studies suggest that inhibition of these kinases may have activity against cancers that do not harbor BRAF mutations. We confirmed NEK9 to be a potent target of dabrafenib by in vitro kinase assays, with inhibition of NEK9 observed in the single-digit nanomolar range. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
NEK9 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261072 |
|
|
Homo sapiens |
1205-Lu Cell |
| pmid |
sentence |
| 29112787 |
We have identified dabrafenib as a potent inhibitor of NEK9 and CDK16, and our studies suggest that inhibition of these kinases may have activity against cancers that do not harbor BRAF mutations. We confirmed NEK9 to be a potent target of dabrafenib by in vitro kinase assays, with inhibition of NEK9 observed in the single-digit nanomolar range. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
dabrafenib | down-regulates activity
chemical inhibition
|
NEK11 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259217 |
|
|
in vitro |
|
| pmid |
sentence |
| 24720932 |
Dabrafenib is known to inhibit V600E, V600K and V600D BRAF enzymes with in vitro IC50 values of 0.65, 0.5 and 1.84 nM, respectively. Dabrafenib can inhibit wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. Other kinases (SIK1, NEK111 and LIMK1) can be inhibited by dabrafenib when administered in high concentrations |
|
| Publications: |
1 |
Organism: |
In Vitro |
3.0
dabrafenib
