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: 60150671
PubChem: 139061047
Guide to Pharmacology: 5711
ChEMBL: CHEMBL1336
ChEMBL: CHEMBL3928540
ChEMBL: CHEMBL1200485
DrugCentral: 2459
LyCHI: 4DAR47Y95JGR
Target Activities
KDR
Vascular endothelial growth factor receptor 2
34 Activities
Items per page:
1 – 10 of 34
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.05 | |||||
Kd | 7.23 | |||||
Ki | 10.68 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
Ki | 9.92 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
IC50 | 9.8 | Bioorg. Med. Chem., (2011) 19:18:5342 | ||||
IC50 | 9.77 | Eur J Med Chem, (2019) 163:None:1 | ||||
IC50 | 9.77 | Eur J Med Chem, (2019) 164:None:440 | ||||
IC50 | 9.35 | Eur J Med Chem, (2017) 127:None:275 | ||||
IC50 | 9.32 | Bioorg. Med. Chem., (2015) 23:13:3228 | ||||
IC50 | 9.32 | Eur. J. Med. Chem., (2015) 103:None:80 | ||||
BRAF
Serine/threonine-protein kinase B-raf
25 Activities
Items per page:
1 – 10 of 25
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.66 | |||||
IC50 | 9 | J. Med. Chem., (2008) 51:22:7049 | ||||
IC50 | 9 | Bioorg. Med. Chem. Lett., (2011) 21:4:1248 | ||||
EC50 | 8.52 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
IC50 | 8.36 | J Med Chem, (2018) 61:14:5775 | ||||
IC50 | 7.92 | Eur. J. Med. Chem., (2014) 87:None:782 | ||||
IC50 | 7.92 | Eur. J. Med. Chem., (2014) 85:None:215 | ||||
IC50 | 7.9 | None, (2015) None:None:None | ||||
IC50 | 7.89 | Bioorg. Med. Chem. Lett., (2013) 23:13:3732 | ||||
IC50 | 7.85 | Bioorg. Med. Chem. Lett., (2008) 18:9:2825 | ||||
FLT3
Receptor-type tyrosine-protein kinase FLT3
25 Activities
Items per page:
1 – 10 of 25
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.24 | |||||
IC50 | 8.89 | Eur J Med Chem, (2019) 176:None:248 | ||||
IC50 | 8.7 | Blood, (2009) 114:14:2984 | ||||
IC50 | 8.7 | J. Med. Chem., (2014) 57:8:3430 | ||||
IC50 | 8.49 | Blood, (2009) 114:14:2984 | ||||
IC50 | 8.4 | J. Med. Chem., (2014) 57:8:3430 | ||||
Kd | 8.35 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.35 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.15 | J. Med. Chem., (2013) 56:4:1641 | ||||
Kd | 7.96 | Nat. Biotechnol., (2008) 26:1:127 | ||||
RAF1
RAF proto-oncogene serine/threonine-protein kinase
20 Activities
Items per page:
1 – 10 of 20
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.22 | |||||
IC50 | 9 | J. Med. Chem., (2008) 51:22:7049 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2008) 18:9:2825 | ||||
Ki | 8.22 | J. Med. Chem., (2008) 51:19:6121 | ||||
IC50 | 8.22 | J. Med. Chem., (2010) 53:4:1413 | ||||
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) 87:None:782 | ||||
IC50 | 8.22 | Eur. J. Med. Chem., (2014) 85:None:215 | ||||
KIT
Mast/stem cell growth factor receptor Kit
13 Activities
Items per page:
1 – 10 of 13
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.17 | |||||
IC50 | 8 | J. Med. Chem., (2008) 51:22:7049 | ||||
Kd | 7.96 | Blood, (2009) 114:14:2984 | ||||
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 | 7.75 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.75 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.75 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
12 Activities
Items per page:
1 – 10 of 12
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.9 | |||||
IC50 | 8.22 | J. Med. Chem., (2015) 58:9:3672 | ||||
Kd | 8.13 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.13 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.13 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.05 | Nat. Chem. Biol., (2008) 4:11:691 | ||||
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 | ||||
Kd | 7.66 | Blood, (2009) 114:14:2984 | ||||
DDR2
Discoidin domain-containing receptor 2
8 Activities
Items per page:
1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8 | |||||
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 | 8.15 | J. Med. Chem., (2014) 57:10:4252 | ||||
Kd | 8.15 | J. Med. Chem., (2014) 57:10:4252 | ||||
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) | ||
|---|---|---|---|---|---|---|
IC50 | 7.7 | |||||
IC50 | 8.52 | Bioorg. Med. Chem., (2010) 18:13:4674 | ||||
Kd | 7.8 | Nat. Biotechnol., (2005) 23:3:329 | ||||
Kd | 7.8 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
IC50 | 7.8 | J. Med. Chem., (2012) 55:12:5749 | ||||
Kd | 7.8 | INHIBITOR | ||||
PDGFRB
Platelet-derived growth factor receptor beta
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.24 | |||||
Ki | 8.4 | None, None:None:None | ||||
IC50 | 8 | J. Med. Chem., (2008) 51:22:7049 | ||||
IC50 | 7.74 | None, (2016) None:None:None | ||||
Kd | 7.43 | INHIBITOR | ||||
EPHX2
Bifunctional epoxide hydrolase 2
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.3 | None, (2015) None:None:None | ||||
IC50 | 9.3 | None, (2015) None:None:None | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2013) 23:13:3732 | ||||
IC50 | 7.92 | None, (2015) None:None:None | ||||
IC50 | 7.92 | |||||
MAP3K20
Mitogen-activated protein kinase kinase kinase 20
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.2 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.2 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.2 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 7.8 | None, None:None:None | ||||
Kd | 8.2 | |||||
DDR1
Epithelial discoidin domain-containing receptor 1
5 Activities
Items per page:
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 | |||||
TEK
Angiopoietin-1 receptor
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.41 | Eur J Med Chem, (2019) 163:None:1 | ||||
IC50 | 9.41 | Eur J Med Chem, (2019) 164:None:440 | ||||
IC50 | 9.08 | Eur J Med Chem, (2017) 127:None:275 | ||||
IC50 | 8.17 | Eur J Med Chem, (2017) 141:None:506 | ||||
IC50 | 8.11 | Eur J Med Chem, (2017) 141:None:373 | ||||
EPHB4
Ephrin type-B receptor 4
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.7 | Eur J Med Chem, (2017) 127:None:275 | ||||
IC50 | 9.66 | Eur J Med Chem, (2019) 163:None:1 | ||||
IC50 | 9.66 | Eur J Med Chem, (2019) 164:None:440 | ||||
IC50 | 8.35 | Eur J Med Chem, (2017) 141:None:506 | ||||
IC50 | 8.34 | Eur J Med Chem, (2017) 141:None:373 | ||||
CSF1R
Macrophage colony-stimulating factor 1 receptor
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.72 | J. Med. Chem., (2008) 51:22:7049 | ||||
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 | ||||
ARAF
Serine/threonine-protein kinase A-Raf
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.15 | Eur J Med Chem, (2017) 130:None:86 | ||||
IC50 | 8.15 | Eur J Med Chem, (2019) 163:None:243 | ||||
IC50 | 7.92 | Bioorg Med Chem Lett, (2019) 29:13:1605 | ||||
IC50 | 8.15 | |||||
HIPK4
Homeodomain-interacting protein kinase 4
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.57 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.48 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8 | None, None:None:None | ||||
Kd | 8.57 | |||||
FGFR1
Fibroblast growth factor receptor 1
2 Activities
FLT1
Vascular endothelial growth factor receptor 1
2 Activities
Items per page: