fedratinib
Ligand Summary
Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera.
UNII: 6L1XP550I6
PubChem: 16722836
Guide to Pharmacology: 5716
ChEMBL: CHEMBL1287853
DrugCentral: 5347
LyCHI: GUJY5FTRMBSB
Target Activities
FLT3
Receptor-type tyrosine-protein kinase FLT3
9 Activities
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1 – 9 of 9
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.31 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.19 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.82 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
Kd | 7.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.54 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.82 | INHIBITOR | ||||
JAK2
Tyrosine-protein kinase JAK2
8 Activities
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1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | |||||
IC50 | 9.12 | J Med Chem, (2021) 64:4.0:2228 | ||||
Kd | 8.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2010) 20:24:7454 | ||||
IC50 | 8.52 | MedChemComm, (2012) 3:1:22 | ||||
IC50 | 8.52 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
IC50 | 8.52 | J Med Chem, (2018) 61:20:9030 | ||||
IC50 | 8.52 | INHIBITOR | ||||
BRD4
Bromodomain-containing protein 4
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.79 | |||||
Kd | 6.79 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
IC50 | 6.54 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
Kd | 6.79 | |||||
JAK1
Tyrosine-protein kinase JAK1
2 Activities
TYK2
Non-receptor tyrosine-protein kinase TYK2
2 Activities
DAPK3
Death-associated protein kinase 3
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.92 | |||||
DAPK2
Death-associated protein kinase 2
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.54 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.54 | |||||
STK16
Serine/threonine-protein kinase 16
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.18 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.18 | |||||
GAK
Cyclin-G-associated kinase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.96 | |||||
MAP3K19
Mitogen-activated protein kinase kinase kinase 19
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.72 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.72 | |||||
DCLK3
Serine/threonine-protein kinase DCLK3
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | |||||
BRDT
Bromodomain testis-specific protein
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 | 6.47 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
IC50 | 6.47 | |||||
Q6ZSR9
Uncharacterized protein FLJ45252
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.56 | Science, (2017) 358:6367:None | ||||
Kd | 6.56 | |||||
DAPK1
Death-associated protein kinase 1
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.8 | |||||
JAK3
Tyrosine-protein kinase JAK3
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 | 6 | |||||
BMP2K
BMP-2-inducible protein 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 | 7.5 | |||||