gilteritinib
Gilteritinib is a small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib demonstrated the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 including FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and it induced apoptosis in leukemic cells expressing FLT3-ITD.
Ligand Summary
UNII: 66D92MGC8M
PubChem: 49803313
Guide to Pharmacology: 8708
ChEMBL: CHEMBL3301603
ChEMBL: CHEMBL3301622
DrugCentral: 5306
LyCHI: S4NDSK8XDGVU
Target Activities
FLT3
Receptor-type tyrosine-protein kinase FLT3
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.39 | None, (2015) None:None:None | ||||
IC50 | 9.39 | None, (2015) None:None:None | ||||
IC50 | 9.52000046 | |||||
IC50 | 8.30103 | INHIBITOR | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.72 | None, (2015) None:None:None | ||||
IC50 | 8.72 | None, (2015) None:None:None | ||||
IC50 | 8.81999969 | |||||
ALK
ALK tyrosine kinase receptor
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.82 | None, (2015) None:None:None | ||||
IC50 | 8.82 | None, (2015) None:None:None | ||||
IC50 | 9.30000019 | |||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.47 | None, (2015) None:None:None | ||||
IC50 | 8.47 | None, (2015) None:None:None | ||||
IC50 | 8.77000046 | |||||
AXL
Tyrosine-protein kinase receptor UFO
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.10000038 | |||||
LTK
Leukocyte tyrosine kinase receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.69999981 | |||||
MERTK
Tyrosine-protein kinase Mer
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52000046 | |||||
NTRK1
High affinity nerve growth factor receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.96000004 | |||||