gilteritinib
Ligand Summary
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.
UNII: 66D92MGC8M
PubChem: 49803313
PubChem: 155520090
Guide to Pharmacology: 8708
ChEMBL: CHEMBL3301622
ChEMBL: CHEMBL4524472
DrugCentral: 5306
LyCHI: S4NDSK8XDGVU
Target Activities
FLT3
Receptor-type tyrosine-protein kinase FLT3
7 Activities
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1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.52 | |||||
IC50 | 9.54 | Eur J Med Chem, (2019) 178:None:468 | ||||
IC50 | 9.39 | None, (2015) None:None:None | ||||
IC50 | 9.39 | None, None:None:None | ||||
IC50 | 9.39 | |||||
Kd | 8.15 | Science, (2017) 358:6367:None | ||||
IC50 | 8.3 | INHIBITOR | ||||
AXL
Tyrosine-protein kinase receptor UFO
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 | 9.1 | |||||
IC50 | 9.14 | Eur J Med Chem, (2019) 178:None:468 | ||||
IC50 | 7.95 | Bioorg Med Chem Lett, (2019) 29:6:836 | ||||
IC50 | 9.1 | INHIBITOR | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
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 | 8.82 | |||||
IC50 | 8.72 | None, (2015) None:None:None | ||||
IC50 | 8.72 | None, None:None:None | ||||
IC50 | 8.72 | |||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
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 | 8.77 | |||||
IC50 | 8.47 | None, (2015) None:None:None | ||||
IC50 | 8.47 | None, None:None:None | ||||
IC50 | 8.47 | |||||
ALK
ALK tyrosine kinase receptor
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.3 | |||||
IC50 | 8.82 | None, (2015) None:None:None | ||||
MERTK
Tyrosine-protein kinase Mer
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | |||||
IC50 | 8.52 | INHIBITOR | ||||
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 | 9.7 | |||||
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 | 8.96 | |||||
AAK1
AP2-associated protein kinase 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Science, (2017) 358:6367:None | ||||
GAK
Cyclin-G-associated kinase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.05 | Science, (2017) 358:6367:None | ||||
ULK3
Serine/threonine-protein kinase ULK3
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.22 | Science, (2017) 358:6367:None | ||||
IRAK3
Interleukin-1 receptor-associated kinase 3
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.15 | Science, (2017) 358:6367:None | ||||
RAN
GTP-binding nuclear protein Ran
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.12 | Science, (2017) 358:6367:None | ||||
ACSL5
Long-chain-fatty-acid--CoA ligase 5
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.68 | Science, (2017) 358:6367:None | ||||
SLC25A6
ADP/ATP translocase 3
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.3 | Science, (2017) 358:6367:None | ||||
Q6ZSR9
Uncharacterized protein FLJ45252
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.96 | Science, (2017) 358:6367:None | ||||
TUFM
Elongation factor Tu, mitochondrial
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.33 | Science, (2017) 358:6367:None | ||||
CYC1
Cytochrome c1, heme protein, mitochondrial
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.7 | Science, (2017) 358:6367:None | ||||
PLK4
Serine/threonine-protein kinase PLK4
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.75 | Science, (2017) 358:6367:None | ||||
SLC25A5
ADP/ATP translocase 2
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.35 | Science, (2017) 358:6367:None | ||||
DHCR24
Delta(24)-sterol reductase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.37 | Science, (2017) 358:6367:None | ||||