sunitinib
Ligand Summary
An indole and pyrrole derivative that inhibits VEGFR-2 and PDGFR BETA RECEPTOR TYROSINE KINASES. It is used as an antineoplastic agent for the treatment of GASTROINTESTINAL STROMAL TUMORS, and for treatment of advanced or metastatic RENAL CELL CARCINOMA.
UNII: V99T50803M
PubChem: 5329102
PubChem: 6456015
Guide to Pharmacology: 5713
ChEMBL: CHEMBL535
ChEMBL: CHEMBL1567
DrugCentral: 2544
LyCHI: T16444CNC2AA
Target Activities
FLT3
Receptor-type tyrosine-protein kinase FLT3
39 Activities
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1 – 10 of 39
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.19 | |||||
Kd | 9.66 | Blood, (2009) 114:14:2984 | ||||
Kd | 9.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.39 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.37 | J Med Chem, (2019) 62:5:2428 | ||||
Kd | 9.33 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.33 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 9.33 | Blood, (2009) 114:14:2984 | ||||
Kd | 9.33 | Blood, (2009) 114:14:2984 | ||||
IC50 | 9.15 | J Med Chem, (2021) 64:8.0:4870 | ||||
KDR
Vascular endothelial growth factor receptor 2
34 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.65 | |||||
Kd | 9.7 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 9.64 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 8.82 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8.54 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2013) 23:20:5630 | ||||
IC50 | 8.33 | Eur J Med Chem, (2018) 158:None:428 | ||||
IC50 | 8.26 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
KIT
Mast/stem cell growth factor receptor Kit
28 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.88 | |||||
Kd | 9.43 | |||||
Kd | 9.68 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.68 | Blood, (2009) 114:14:2984 | ||||
Kd | 9.68 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.55 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.55 | Blood, (2009) 114:14:2984 | ||||
Kd | 9.55 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.43 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.43 | Blood, (2009) 114:14:2984 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
16 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.1 | |||||
IC50 | 8.2 | |||||
Kd | 10.12 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 10.12 | Blood, (2009) 114:14:2984 | ||||
Kd | 10.12 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.7 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 9.68 | Nat. Biotechnol., (2005) 23:3:329 | ||||
IC50 | 8.7 | J. Med. Chem., (2003) 46:7:1116 | ||||
IC50 | 8.7 | J Med Chem, (2017) 60:1:248 | ||||
Kd | 8.4 | Science, (2017) 358:6367:None | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
12 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.8 | |||||
Kd | 8.24 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.24 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.06 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.06 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.92 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.92 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.72 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.72 | Blood, (2009) 114:14:2984 | ||||
TNIK
TRAF2 and NCK-interacting protein kinase
7 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 7.6 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 7.6 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.6 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | MedChemComm, (2015) 6:8:1564 | ||||
Kd | 7.6 | |||||
FLT1
Vascular endothelial growth factor receptor 1
6 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9 | Bioorg. Med. Chem. Lett., (2012) 22:15:4979 | ||||
Kd | 8.74 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.74 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.74 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8.7 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
IC50 | 7.23 | INHIBITOR | ||||
STK17A
Serine/threonine-protein kinase 17A
6 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 9 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9 | Blood, (2009) 114:14:2984 | ||||
Kd | 9 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.68 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 7.68 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 9 | |||||
AXL
Tyrosine-protein kinase receptor UFO
6 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.05 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.05 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.05 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.05 | J. Med. Chem., (2016) 59:8:3593 | ||||
IC50 | 8.05 | Bioorg Med Chem Lett, (2017) 27:16:3766 | ||||
Kd | 8.05 | |||||
CSF1R
Macrophage colony-stimulating factor 1 receptor
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.7 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.7 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2008) 18:17:4794 | ||||
Kd | 8.7 | INHIBITOR | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.6 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
IC50 | 6.3 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
IC50 | 6.3 | Eur J Med Chem, (2017) 127:None:72 | ||||
IC50 | 5.1 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
IC50 | 5 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
PDGFRA
Platelet-derived growth factor receptor alpha
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 9.1 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.1 | Blood, (2009) 114:14:2984 | ||||
Kd | 9.1 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.56 | J Med Chem, (2021) 64:8.0:4870 | ||||
IC50 | 6.96 | INHIBITOR | ||||
AAK1
AP2-associated protein kinase 1
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.96 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.96 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | J Med Chem, (2019) 62:12:5810 | ||||
Kd | 7.96 | |||||
CLK4
Dual specificity protein kinase CLK4
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.54 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.54 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.54 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.54 | Eur J Med Chem, (2017) 126:None:754 | ||||
Kd | 7.54 | |||||
CLK1
Dual specificity protein kinase CLK1
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.66 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.66 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.66 | Eur J Med Chem, (2017) 126:None:754 | ||||
Kd | 7.66 | |||||
CLK2
Dual specificity protein kinase CLK2
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.7 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.7 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | Eur J Med Chem, (2017) 126:None:754 | ||||
Kd | 7.7 | |||||
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 | 8.05 | |||||
IC50 | 8.05 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
Ki | 7.77 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
Ki | 7.77 | INHIBITOR | ||||
PHKG2
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.23 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.23 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.23 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.23 | |||||
DAPK3
Death-associated protein kinase 3
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.66 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.66 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.66 | |||||
CSNK1D
Casein kinase I isoform delta
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.82 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.82 | |||||
PAK3
Serine/threonine-protein kinase PAK 3
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.8 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.8 | |||||
RPS6KA2
Ribosomal protein S6 kinase alpha-2
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.77 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.77 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.55 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.77 | |||||
STK10
Serine/threonine-protein kinase 10
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.72 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.72 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.72 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.72 | |||||
PHKG1
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.26 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.26 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.26 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.26 | |||||
RPS6KA5
Ribosomal protein S6 kinase alpha-5
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.77 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.55 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.55 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.77 | |||||
GAK
Cyclin-G-associated kinase
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.7 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.7 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | |||||
BMP2K
BMP-2-inducible protein kinase
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.26 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.26 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.26 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.26 | |||||
STK4
Serine/threonine-protein kinase 4
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.72 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.72 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.72 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.72 | |||||
MERTK
Tyrosine-protein kinase Mer
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.58 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.58 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.58 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.59 | |||||
MYLK4
Myosin light chain kinase family member 4
4 Activities
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