sorafenib
Sorafenib is a kinase inhibitor that decreases tumor cell proliferation in vitro. Sorafenib was shown to inhibit multiple intracellular (c-CRAF, BRAF and mutant BRAF) and cell surface kinases (KIT, FLT-3, RET, RET/PTC, VEGFR-1, VEGFR-2, VEGFR-3, and PDGFR-beta). Several of these kinases are thought to be involved in tumor cell signaling, angiogenesis and apoptosis. Sorafenib inhibited tumor growth of HCC, RCC, and DTC human tumor xenografts in immunocompromised mice. Reductions in tumor angiogenesis were seen in models of HCC and RCC upon sorafenib treatment, and increases in tumor apoptosis were observed in models of hepatocellular carcinoma, renal cell carcinoma, and differentiated thyroid carcinoma.
Ligand Summary
UNII: 9ZOQ3TZI87
PubChem: 216239
PubChem: 25058195
Guide to Pharmacology: 5711
ChEMBL: CHEMBL1336
ChEMBL: CHEMBL1200485
DrugCentral: 2459
LyCHI: 4DAR47Y95JGR
Target Activities
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1 – 10 of 21
KDR
Vascular endothelial growth factor receptor 2
24 Activities
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1 – 10 of 24
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.57 | Nat. Chem. Biol., (2008) 4:11:691 | ||||
IC50 | 7.64 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
Ki | 7.66 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
IC50 | 7.66 | Eur. J. Med. Chem., (2012) 53:None:254 | ||||
IC50 | 7.7 | Bioorg. Med. Chem., (2013) 21:11:2856 | ||||
IC50 | 7.7 | Bioorg. Med. Chem. Lett., (2012) 22:14:4654 | ||||
IC50 | 7.9 | Eur. J. Med. Chem., (2014) 72:None:146 | ||||
IC50 | 7.96 | None, (2016) None:None:None | ||||
IC50 | 8 | Eur. J. Med. Chem., (2016) 109:None:371 | ||||
IC50 | 8.21 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
FLT3
Receptor-type tyrosine-protein kinase FLT3
19 Activities
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1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.7 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 7.7 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 7.77 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.89 | MedChemComm, (2016) 7:3:484 | ||||
Kd | 7.89 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.89 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.89 | J. Med. Chem., (2009) 52:23:7808 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | Nat. Biotechnol., (2008) 26:1:127 | ||||
RAF1
RAF proto-oncogene serine/threonine-protein kinase
16 Activities
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1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.61 | Bioorg. Med. Chem., (2012) 20:14:4323 | ||||
IC50 | 7.66 | Eur. J. Med. Chem., (2014) 77:None:351 | ||||
IC50 | 7.92 | Eur. J. Med. Chem., (2009) 44:3:1240 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2004) 14:3:783 | ||||
Ki | 8.22 | J. Med. Chem., (2008) 51:19:6121 | ||||
IC50 | 8.22 | Bioorg. Med. Chem. Lett., (2010) 20:19:5722 | ||||
IC50 | 8.22 | J. Med. Chem., (2011) 54:6:1836 | ||||
IC50 | 8.22 | J. Med. Chem., (2012) 55:17:7332 | ||||
IC50 | 8.22 | Eur. J. Med. Chem., (2014) 85:None:215 | ||||
IC50 | 8.22 | Eur. J. Med. Chem., (2016) 115:None:201 | ||||
BRAF
Serine/threonine-protein kinase B-raf
12 Activities
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1 – 10 of 12
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.58 | Eur. J. Med. Chem., (2015) 89:None:581 | ||||
Ki | 7.66 | Chem. Biol., (2005) 12:6:621 | ||||
IC50 | 7.66 | Bioorg. Med. Chem. Lett., (2011) 21:23:6941 | ||||
IC50 | 7.66 | J. Med. Chem., (2012) 55:17:7332 | ||||
IC50 | 7.66 | Nat. Chem. Biol., (2006) 2:7:358 | ||||
IC50 | 7.82 | Bioorg. Med. Chem. Lett., (2008) 18:9:2825 | ||||
IC50 | 7.9 | None, (2015) None:None:None | ||||
IC50 | 7.92 | Eur. J. Med. Chem., (2014) 85:None:215 | ||||
IC50 | 7.92 | Eur. J. Med. Chem., (2014) 87:None:782 | ||||
EC50 | 8.52 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
10 Activities
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1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.89 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.05 | Nat. Chem. Biol., (2008) 4:11:691 | ||||
Kd | 8.13 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.13 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.22 | J. Med. Chem., (2015) 58:9:3672 | ||||
IC50 | 7.9000001 | |||||
Kd | 8.13 | INHIBITOR | ||||
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) | ||
|---|---|---|---|---|---|---|
Kd | 7.55 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.75 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.75 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.8 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8 | J. Med. Chem., (2008) 51:22:7049 | ||||
IC50 | 7.17000008 | |||||
Kd | 7.8 | INHIBITOR | ||||
DDR2
Discoidin domain-containing 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) | ||
|---|---|---|---|---|---|---|
IC50 | 8.15 | J. Med. Chem., (2014) 57:10:4252 | ||||
Kd | 8.15 | J. Med. Chem., (2014) 57:10:4252 | ||||
Kd | 8.18 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.18 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.18 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.18 | J. Med. Chem., (2015) 58:8:3287 | ||||
IC50 | 8 | |||||
Kd | 8.18 | |||||
FLT4
Vascular endothelial growth factor receptor 3
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
Kd | 7.8 | Nat. Biotechnol., (2005) 23:3:329 | ||||
IC50 | 7.8 | J. Med. Chem., (2012) 55:12:5749 | ||||
IC50 | 8.52 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
IC50 | 7.69999981 | |||||
Kd | 7.8 | INHIBITOR | ||||
DDR1
Epithelial discoidin domain-containing receptor 1
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
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 | ||||
Kd | 8.82 | J. Med. Chem., (2015) 58:8:3287 | ||||
Kd | 8.82 | |||||
CSF1R
Macrophage colony-stimulating factor 1 receptor
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 | 7.55 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.55 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.55 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.72 | J. Med. Chem., (2008) 51:22:7049 | ||||