pazopanib
Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR)-1 and -3, cytokine receptor (Kit), interleukin-2 receptor-inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice.
Ligand Summary
UNII: 7RN5DR86CK
PubChem: 11525740
PubChem: 10113978
Guide to Pharmacology: 5698
ChEMBL: CHEMBL1201733
ChEMBL: CHEMBL477772
DrugCentral: 4118
LyCHI: VAD1FZTYS37A
Target Activities
KIT
Mast/stem cell growth factor receptor Kit
10 Activities
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1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.8499999 | |||||
Kd | 8.74 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.64 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.64 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.55 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.55 | Eur. J. Med. Chem., (2011) 46:6:2043 | ||||
Kd | 8.55 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.19 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.19 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.74 | INHIBITOR | ||||
KDR
Vascular endothelial growth factor receptor 2
8 Activities
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1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8499999 | |||||
IC50 | 7.51999998 | |||||
Ki | 8.5 | None, None:None:None | ||||
IC50 | 8.3 | J. Med. Chem., (2013) 56:17:6991 | ||||
IC50 | 8.1 | J. Med. Chem., (2008) 51:15:4632 | ||||
Kd | 7.85 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.85 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.85 | INHIBITOR | ||||
FLT1
Vascular endothelial growth factor receptor 1
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 | 8 | |||||
IC50 | 8 | J. Med. Chem., (2008) 51:15:4632 | ||||
IC50 | 8 | Eur J Med Chem, (2019) 179:None:916 | ||||
Kd | 7.85 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.85 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 7.8 | None, None:None:None | ||||
Kd | 7.85 | INHIBITOR | ||||
CSF1R
Macrophage colony-stimulating factor 1 receptor
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.84000015 | |||||
Kd | 8.1 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.1 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 7.7 | None, None:None:None | ||||
Kd | 8.1 | INHIBITOR | ||||
PDGFRB
Platelet-derived growth factor receptor beta
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.07999992 | |||||
Kd | 8.7 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8.4 | None, None:None:None | ||||
Kd | 8.7 | INHIBITOR | ||||
FLT4
Vascular endothelial growth factor receptor 3
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.32999992 | |||||
Kd | 7.57 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.57 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.57 | INHIBITOR | ||||
PDGFRA
Platelet-derived growth factor receptor alpha
3 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.31 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.31 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.31 | INHIBITOR | ||||
FGFR1
Fibroblast growth factor receptor 1
2 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.13000011 | |||||
Kd | 6 | INHIBITOR | ||||
ACHE
Acetylcholinesterase
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.03 | J. Med. Chem., (2016) 59:9:4121 | ||||
LCK
Tyrosine-protein kinase Lck
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 5.92 | INHIBITOR | ||||
FGFR3
Fibroblast growth factor receptor 3
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 | 6.21 | INHIBITOR | ||||
ITK
Tyrosine-protein kinase ITK/TSK
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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INHIBITOR | ||||||