Molecule Details
InChIKeyRITAVMQDGBJQJZ-FMIVXFBMSA-N
Compound NameAxitinib
Canonical SMILESCNC(=O)c1ccccc1Sc1ccc2c(/C=C/c3ccccn3)n[nH]c2c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)43
Pfam Stratification Cross-Family
Avg pChEMBL7.07
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB06626
Drug NameAxitinib
CAS Number319460-85-0
Groups approved investigational
ATC Codes L01EK01
DescriptionAxitinib is a second generation tyrosine kinase inhibitor that works by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3).[L6676] Through this mechanism of action, axitinib blocks angiogenesis, tumour growth and metastases. It is reported to exhibit pote...

Categories: Acids, Carbocyclic Amides Antineoplastic Agents Antineoplastic and Immunomodulating Agents Benzamides and benzamide derivatives Benzene Derivatives Benzoates Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2C19 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP3A5 Substrates Cytochrome P-450 CYP3A5 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Substrates Enzyme Inhibitors Heterocyclic Compounds, Fused-Ring Indazoles Kinase Inhibitor Narrow Therapeutic Index Drugs OATP1B1/SLCO1B1 Inhibitors OATP1B1/SLCO1B1 Substrates P-glycoprotein inhibitors P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Protein Kinase Inhibitors Pyrazoles Receptor Tyrosine Kinase Inhibitors Tyrosine Kinase Inhibitors UGT1A1 Substrates UGT1A1 Substrates with a Narrow Therapeutic Index Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
Cross-references: BindingDB: 25117 ChEBI: 66910 CHEMBL1289926 ChemSpider: 4953153 Drugs Product Database (DPD): 21398 D03218 PDB: AXI PharmGKB: PA164924493 PubChem:6450551 PubChem:347827779 RxCUI: 1242999 Wikipedia: Axitinib ZINC: ZINC000003816287
Target Activities (43)
Target Gene Organism Category Pfam pChEMBL Type Source
P17948 FLT1 Homo sapiens Human PF07679 PF00047 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 10.0 IC50 ChEMBL;BindingDB
P35916 FLT4 Homo sapiens Human PF07679 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 10.0 IC50 ChEMBL;BindingDB
P35968 KDR Homo sapiens Human PF07679 PF00047 PF13895 PF22971 PF07714 PF21339 PF17988 PF22854 9.7 IC50 ChEMBL;BindingDB
P16234 PDGFRA Homo sapiens Human PF07679 PF25305 PF07714 9.3 Kd ChEMBL;BindingDB
P09619 PDGFRB Homo sapiens Human PF00047 PF13927 PF25305 PF07714 9.0 Kd ChEMBL;BindingDB
Q9UQB9 AURKC Homo sapiens Human PF00069 8.9 Kd ChEMBL;BindingDB
P10721 KIT Homo sapiens Human PF00047 PF07714 8.5 Kd ChEMBL;BindingDB
Q96GD4 AURKB Homo sapiens Human PF00069 8.0 Kd ChEMBL;BindingDB
O00444 PLK4 Homo sapiens Human PF00069 PF18190 PF18409 7.8 IC50 ChEMBL;BindingDB
P07333 CSF1R Homo sapiens Human PF00047 PF25305 PF07714 7.7 Kd ChEMBL;BindingDB
P00519 ABL1 Homo sapiens Human PF08919 PF07714 PF00017 PF00018 7.4 Kd ChEMBL;BindingDB
P42684 ABL2 Homo sapiens Human PF08919 PF07714 PF00017 PF00018 7.2 Kd ChEMBL;BindingDB
O14965 AURKA Homo sapiens Human PF00069 7.1 Kd ChEMBL;BindingDB
P35590 TIE1 Homo sapiens Human PF00041 PF00047 PF07714 7.0 Kd ChEMBL;BindingDB
P07949 RET Homo sapiens Human PF00028 PF07714 PF17756 PF17812 PF17813 PF22540 7.0 Kd ChEMBL;BindingDB
P21802 FGFR2 Homo sapiens Human PF07679 PF13927 PF07714 7.0 Kd ChEMBL;BindingDB
Q13163 MAP2K5 Homo sapiens Human PF00564 PF00069 6.8 Kd ChEMBL;BindingDB
Q13470 TNK1 Homo sapiens Human PF07714 PF22931 6.8 Kd ChEMBL;BindingDB
Q9UKE5 TNIK Homo sapiens Human PF00780 PF00069 6.7 Kd ChEMBL;BindingDB
P11274 BCR Homo sapiens Human PF09036 PF00168 PF19057 PF00620 PF00621 6.7 Kd ChEMBL
P22607 FGFR3 Homo sapiens Human PF21165 PF07679 PF13927 PF07714 6.7 Kd ChEMBL;BindingDB
P36888 FLT3 Homo sapiens Human PF00047 PF07714 6.7 Kd ChEMBL;BindingDB
Q56UN5 MAP3K19 Homo sapiens Human PF00069 6.6 Kd ChEMBL;BindingDB
Q02763 TEK Homo sapiens Human PF00041 PF10430 PF07714 6.5 Kd ChEMBL;BindingDB
P11362 FGFR1 Homo sapiens Human PF07679 PF00047 PF07714 6.5 Kd ChEMBL;BindingDB
Q92918 MAP4K1 Homo sapiens Human PF00780 PF00069 6.5 Kd ChEMBL;BindingDB
Q08345 DDR1 Homo sapiens Human PF21114 PF00754 PF07714 6.5 Kd ChEMBL;BindingDB
O95819 MAP4K4 Homo sapiens Human PF00780 PF00069 6.5 Kd ChEMBL;BindingDB
O15197 EPHB6 Homo sapiens Human PF14575 PF25599 PF01404 PF07699 PF00041 PF07714 PF07647 6.4 Kd ChEMBL;BindingDB
O75716 STK16 Homo sapiens Human PF00069 6.4 Kd ChEMBL;BindingDB
Q9UBN7 HDAC6 Homo sapiens Human PF00850 PF02148 6.4 IC50 ChEMBL
P30530 AXL Homo sapiens Human PF00041 PF13927 PF07714 6.4 Kd ChEMBL;BindingDB
Q9UHD2 TBK1 Homo sapiens Human PF00069 PF18394 PF18396 6.3 IC50 BindingDB
Q92772 CDKL2 Homo sapiens Human PF00069 6.3 Kd ChEMBL;BindingDB
Q9Y4K4 MAP4K5 Homo sapiens Human PF00780 PF00069 6.3 Kd ChEMBL;BindingDB
Q8N4C8 MINK1 Homo sapiens Human PF00780 PF00069 6.2 Kd ChEMBL;BindingDB
P09769 FGR Homo sapiens Human PF07714 PF00017 PF00018 6.2 Kd ChEMBL
Q6PHR2 ULK3 Homo sapiens Human PF04212 PF00069 6.2 Kd ChEMBL;BindingDB
P08581 MET Homo sapiens Human PF07714 PF01437 PF01403 PF01833 6.0 Kd ChEMBL;BindingDB
Q5S007 LRRK2 Homo sapiens Human PF23745 PF23744 PF23748 PF16095 PF25497 PF13855 PF00069 PF08477 6.0 Kd ChEMBL;BindingDB
O14730 RIOK3 Homo sapiens Human PF01163 6.0 Kd ChEMBL;BindingDB
Q9H2G2 SLK Homo sapiens Human PF00069 PF12474 6.0 Kd ChEMBL;BindingDB
Q9NSY1 BMP2K Homo sapiens Human PF15282 PF00069 6.0 Kd ChEMBL;BindingDB
DrugBank Target Actions (13)
Target Gene Target Name Action Type
P05177 CYP1A2 Cytochrome P450 1A2 substrate enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P20815 CYP3A5 Cytochrome P450 3A5 substrate enzymes
P22309 UGT1A1 UDP-glucuronosyltransferase 1A1 substrate enzymes
P33261 CYP2C19 Cytochrome P450 2C19 substrate enzymes
P00519 ABL1 Tyrosine-protein kinase ABL1 inhibitor targets
P17948 FLT1 Vascular endothelial growth factor receptor 1 inhibitor targets
P35916 FLT4 Vascular endothelial growth factor receptor 3 inhibitor targets
P35968 KDR Vascular endothelial growth factor receptor 2 inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
Q9Y6L6 SLCO1B1 Solute carrier organic anion transporter family member 1B1 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q9Y6L6 SLCO1B1 Solute carrier organic anion transporter family member 1B1 substrate transporters