quizartinib
Quizartinib is the most selective type II FLT3 inhibitor and has shown the strongest single-agent activity in patient population with R/R-AML (acute myeloid leukemia) with FLT3 mutations. The FLT3 tyrosine kinase inhibitors act as direct inhibitors of FLT3 via competitive inhibition of ATP-binding sites in the FLT3 receptor. Type II FLT3 inhibitors bind the FLT3 receptor in the inactive conformation in a region adjacent to the ATP-binding domain. As a result of this binding affinity, these inhibitors prevent activity of ITD (the internal tandem duplication) mutations but do not target TKD (the tyrosine kinase domain) mutations
Ligand Summary
UNII: 7LA4O6Q0D3
PubChem: 24889392
Guide to Pharmacology: 5658
ChEMBL: CHEMBL576982
DrugCentral: 5341
LyCHI: 9PMFT71R1QVA
Target Activities
FLT3
Receptor-type tyrosine-protein kinase FLT3
39 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.38 | |||||
IC50 | 9.1 | Blood, (2009) 114:14:2984 | ||||
IC50 | 8.96 | Blood, (2009) 114:14:2984 | ||||
IC50 | 8.96 | Eur J Med Chem, (2019) 184:None:111710 | ||||
Kd | 8.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.89 | J Med Chem, (2019) 62:5:2428 | ||||
Kd | 8.89 | J Med Chem, (2016) 59:13:6187 | ||||
Kd | 8.89 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
Kd | 8.8 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 8.8 | Blood, (2009) 114:14:2984 | ||||
KIT
Mast/stem cell growth factor receptor Kit
14 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 8.32 | |||||
Kd | 8.8 | J. Med. Chem., (2010) 53:19:6779 | ||||
Kd | 8.44 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.34 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
Kd | 8.32 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 8.32 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.32 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.32 | J Med Chem, (2017) 60:20:8407 | ||||
Kd | 8.3 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.3 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
13 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 8 | |||||
Kd | 8.8 | J. Med. Chem., (2010) 53:19:6779 | ||||
Kd | 8.52 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.52 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.42 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
Kd | 8.1 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.04 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.04 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 8 | Blood, (2009) 114:14:2984 | ||||
CSF1R
Macrophage colony-stimulating factor 1 receptor
7 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 7.92 | |||||
Kd | 8.8 | J. Med. Chem., (2010) 53:19:6779 | ||||
Kd | 8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.92 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 7.92 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.92 | J Med Chem, (2017) 60:20:8407 | ||||
Kd | 7.82 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
PDGFRA
Platelet-derived growth factor receptor alpha
7 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 7.96 | |||||
Kd | 8.8 | J. Med. Chem., (2010) 53:19:6779 | ||||
Kd | 8.12 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
Kd | 7.96 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 7.96 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | J Med Chem, (2017) 60:20:8407 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
7 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 8.11 | |||||
Kd | 8.8 | J. Med. Chem., (2010) 53:19:6779 | ||||
Kd | 8.4 | ACS Med Chem Lett, (2020) 11:8:1567 | ||||
Kd | 8.11 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 8.11 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.11 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.11 | J Med Chem, (2017) 60:20:8407 | ||||
MYH10
Myosin-10
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 6.12 | Science, (2017) 358:6367:None | ||||