sunitinib
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.
Ligand Summary
UNII: V99T50803M
PubChem: 5329102
PubChem: 6456015
Guide to Pharmacology: 5713
ChEMBL: CHEMBL535
ChEMBL: CHEMBL1567
DrugCentral: 2544
LyCHI: T16444CNC2AA
Target Activities
KDR
Vascular endothelial growth factor receptor 2
28 Activities
Items per page:
1 – 10 of 28
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.57 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
IC50 | 7.6 | Bioorg. Med. Chem. Lett., (2008) 18:9:2793 | ||||
IC50 | 7.65 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
IC50 | 7.72 | Bioorg. Med. Chem., (2014) 22:14:3753 | ||||
IC50 | 7.72 | Bioorg. Med. Chem., (2015) 23:10:2408 | ||||
IC50 | 7.72 | ACS Med. Chem. Lett., (2014) 5:5:480 | ||||
IC50 | 7.75 | J. Med. Chem., (2005) 48:19:6066 | ||||
IC50 | 7.75 | Bioorg. Med. Chem. Lett., (2007) 17:8:2126 | ||||
IC50 | 7.75 | Eur. J. Med. Chem., (2016) 108:None:495 | ||||
IC50 | 7.82 | J. Med. Chem., (2010) 53:22:8140 | ||||
FLT3
Receptor-type tyrosine-protein kinase FLT3
25 Activities
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1 – 10 of 25
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.68 | J. Med. Chem., (2010) 53:4:1413 | ||||
IC50 | 7.8 | Bioorg. Med. Chem. Lett., (2010) 20:20:6129 | ||||
Kd | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8 | Blood, (2009) 114:14:2984 | ||||
IC50 | 8.1 | J. Med. Chem., (2012) 55:2:725 | ||||
IC50 | 8.19 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
Kd | 8.37 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.37 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2010) 20:20:6129 | ||||
Kd | 8.62 | Nat. Biotechnol., (2008) 26:1:127 | ||||
KIT
Mast/stem cell growth factor receptor Kit
22 Activities
Items per page:
1 – 10 of 22
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.88 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
IC50 | 8 | J. Med. Chem., (2010) 53:4:1413 | ||||
IC50 | 8.05 | Bioorg. Med. Chem. Lett., (2013) 23:20:5630 | ||||
IC50 | 8.1 | J. Med. Chem., (2012) 55:2:725 | ||||
Ki | 8.4 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
Kd | 8.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9.15 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 9.15 | Nat. Biotechnol., (2005) 23:3:329 | ||||
IC50 | 9.15 | J. Med. Chem., (2013) 56:14:5757 | ||||
Kd | 9.39 | Nat. Biotechnol., (2008) 26:1:127 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
13 Activities
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1 – 10 of 13
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.77 | Bioorg. Med. Chem. Lett., (2010) 20:20:6129 | ||||
IC50 | 7.97 | Bioorg. Med. Chem. Lett., (2013) 23:20:5630 | ||||
IC50 | 8.05 | J. Med. Chem., (2010) 53:22:8140 | ||||
Ki | 8.1 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
IC50 | 8.7 | J. Med. Chem., (2003) 46:7:1116 | ||||
Kd | 9.68 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 9.7 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
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 | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
9 Activities
Items per page:
1 – 9 of 9
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 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.92 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.92 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.06 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.24 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.80000019 | |||||
IC50 | 8.8 | INHIBITOR | ||||
TNIK
TRAF2 and NCK-interacting protein kinase
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 7.6 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 7.6 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.6 | MedChemComm, (2015) 6:8:1564 | ||||
Kd | 7.6 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | |||||
STK17A
Serine/threonine-protein kinase 17A
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.68 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 7.68 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 9 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9 | Blood, (2009) 114:14:2984 | ||||
Kd | 9 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 9 | |||||
FLT1
Vascular endothelial growth factor receptor 1
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.7 | Eur. J. Med. Chem., (2014) 82:None:139 | ||||
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 | ||||