FAMITINIB


Active Pharmaceutical Ingredients Bioactive chemicals	Exact Similarity SubStructure	Threshold (%) >= 70


InChI Key	GKEYKDOLBLYGRB-LGMDPLHJSA-N
Smiles	CCN(CC)CCN1CCc2[nH]c(/C=C3\C(=O)Nc4ccc(F)cc43)c(C)c2C1=O
InChI	InChI=1S/C23H27FN4O2/c1-4-27(5-2)10-11-28-9-8-19-21(23(28)30)14(3)20(25-19)13-17-16-12-15(24)6-7-18(16)26-22(17)29/h6-7,12-13,25H,4-5,8-11H2,1-3H3,(H,26,29)/b17-13-

Mechanism of Action	Action	Reference
Platelet-derived growth factor receptor inhibitor	INHIBITOR	DOI PubMed ClinicalTrials


Protein: Platelet-derived growth factor receptor Description: Platelet-derived growth factor receptor beta Organism : Homo sapiens P09619 ENSG00000113721











Protein: Stem cell growth factor receptor Description: Mast/stem cell growth factor receptor Kit Organism : Homo sapiens P10721 ENSG00000157404











Protein: Platelet-derived growth factor receptor Description: Platelet-derived growth factor receptor alpha Organism : Homo sapiens P16234 ENSG00000134853











Protein: Vascular endothelial growth factor receptor 1 Description: Vascular endothelial growth factor receptor 1 Organism : Homo sapiens P17948 ENSG00000102755











Protein: Vascular endothelial growth factor receptor 3 Description: Vascular endothelial growth factor receptor 3 Organism : Homo sapiens P35916 ENSG00000037280











Protein: Vascular endothelial growth factor receptor 2 Description: Vascular endothelial growth factor receptor 2 Organism : Homo sapiens P35968 ENSG00000128052











Protein: Tyrosine-protein kinase receptor FLT3 Description: Receptor-type tyrosine-protein kinase FLT3 Organism : Homo sapiens P36888 ENSG00000122025

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase PDGFR family	-	2	-	-	-
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase VEGFR family	-	2-5	-	-	-

Assay Description	Organism	Bioactivity
Inhibition of c-Kit after 30 mins by ELISA	None	2.0 nM
Inhibition of human VEGFR2 after 30 mins by ELISA	Homo sapiens	5.0 nM
Inhibition of human PDGFRbeta after 30 mins by ELISA	Homo sapiens	4.0 nM
Inhibition of VEGFR2-induced cell proliferation in HUVEC after 72 hrs by sulforhodamine B method	Homo sapiens	2.0 nM

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