Molecule Details
| InChIKey | CUIHSIWYWATEQL-UHFFFAOYSA-N |
|---|---|
| Compound Name | Pazopanib |
| Canonical SMILES | Cc1ccc(Nc2nccc(N(C)c3ccc4c(C)n(C)nc4c3)n2)cc1S(N)(=O)=O |
| Clinical Status | Clinical Multi-Target |
| Targets (Human+Pathogen) | 61 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 6.68 |
| Source | BindingDB;ChEMBL;TTD_MultiTarget |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB06589 |
|---|---|
| Drug Name | Pazopanib |
| CAS Number | 444731-52-6 |
| Groups | approved investigational |
| ATC Codes | L01EX03 |
| Description | Pazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009. |
Categories: Amides Angiogenesis Inhibitors Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Substrates Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP2C8 Inhibitors Cytochrome P-450 CYP2C8 Inhibitors (weak) Cytochrome P-450 CYP2C8 Substrates Cytochrome P-450 CYP2C8 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (weak) Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Hepatotoxic Agents Heterocyclic Compounds, Fused-Ring Immunosuppressive Agents Kinase Inhibitor Moderate Risk QTc-Prolonging Agents Narrow Therapeutic Index Drugs OATP1B1/SLCO1B1 Inhibitors P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Protein Kinase Inhibitors Pyrazoles QTc Prolonging Agents Receptors, Vascular Endothelial Growth Factor, antagonists & inhibitors Sulfones Sulfur Compounds Tyrosine Kinase Inhibitors UGT1A1 Inhibitors
Cross-references: BindingDB: 26474 ChEBI: 71219 CHEMBL477772 ChemSpider: 8289501 Drugs Product Database (DPD): 20595 D05380 PubChem:10113978 PubChem:175427074 RxCUI: 714438 Wikipedia: Pazopanib ZINC: ZINC000011617039
Target Activities (61)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| O43570 | CA12 | Homo sapiens | Human | PF00194 | 9.1 | Ki | ChEMBL |
| P16234 | PDGFRA | Homo sapiens | Human | PF07679 PF25305 PF07714 | 8.3 | Kd | ChEMBL;BindingDB |
| P07333 | CSF1R | Homo sapiens | Human | PF00047 PF25305 PF07714 | 8.1 | Kd | ChEMBL;BindingDB |
| P11362 | FGFR1 | Homo sapiens | Human | PF07679 PF00047 PF07714 | 8.1 | pIC50 | TTD_MultiTarget |
| Q16790 | CA9 | Homo sapiens | Human | PF00194 | 8.0 | Ki | ChEMBL;BindingDB |
| P00915 | CA1 | Homo sapiens | Human | PF00194 | 7.9 | Ki | ChEMBL |
| P17948 | FLT1 | Homo sapiens | Human | PF07679 PF00047 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 | 7.8 | IC50 | ChEMBL;BindingDB |
| P09619 | PDGFRB | Homo sapiens | Human | PF00047 PF13927 PF25305 PF07714 | 7.7 | Kd | ChEMBL;BindingDB |
| P10721 | KIT | Homo sapiens | Human | PF00047 PF07714 | 7.5 | Kd | ChEMBL;BindingDB |
| P35968 | KDR | Homo sapiens | Human | PF07679 PF00047 PF13895 PF22971 PF07714 PF21339 PF17988 PF22854 | 7.5 | IC50 | ChEMBL;BindingDB |
| P00918 | CA2 | Homo sapiens | Human | PF00194 | 7.5 | Ki | ChEMBL |
| Q9H2K8 | TAOK3 | Homo sapiens | Human | PF00069 | 7.3 | Kd | ChEMBL;BindingDB |
| P35916 | FLT4 | Homo sapiens | Human | PF07679 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 | 7.3 | IC50 | ChEMBL;BindingDB |
| Q08345 | DDR1 | Homo sapiens | Human | PF21114 PF00754 PF07714 | 7.2 | Kd | ChEMBL;BindingDB |
| O15197 | EPHB6 | Homo sapiens | Human | PF14575 PF25599 PF01404 PF07699 PF00041 PF07714 PF07647 | 7.1 | Kd | ChEMBL;BindingDB |
| O94804 | STK10 | Homo sapiens | Human | PF00069 PF12474 | 7.1 | Kd | ChEMBL;BindingDB |
| Q16832 | DDR2 | Homo sapiens | Human | PF21114 PF00754 PF07714 | 7.0 | Kd | ChEMBL;BindingDB |
| P33981 | TTK | Homo sapiens | Human | PF00069 | 6.8 | Kd | ChEMBL;BindingDB |
| O14976 | GAK | Homo sapiens | Human | PF00069 PF10409 | 6.7 | Kd | ChEMBL;BindingDB |
| P21802 | FGFR2 | Homo sapiens | Human | PF07679 PF13927 PF07714 | 6.7 | Kd | ChEMBL;BindingDB |
| Q7L7X3 | TAOK1 | Homo sapiens | Human | PF00069 | 6.6 | Kd | ChEMBL;BindingDB |
| Q9H2G2 | SLK | Homo sapiens | Human | PF00069 PF12474 | 6.6 | Kd | ChEMBL;BindingDB |
| Q13546 | RIPK1 | Homo sapiens | Human | PF00531 PF07714 | 6.6 | Kd | ChEMBL;BindingDB |
| P07949 | RET | Homo sapiens | Human | PF00028 PF07714 PF17756 PF17812 PF17813 PF22540 | 6.6 | Kd | ChEMBL;BindingDB |
| Q8TBX8 | PIP4K2C | Homo sapiens | Human | PF01504 | 6.5 | Kd | ChEMBL;BindingDB |
| O00444 | PLK4 | Homo sapiens | Human | PF00069 PF18190 PF18409 | 6.5 | Kd | ChEMBL;BindingDB |
| P80192 | MAP3K9 | Homo sapiens | Human | PF07714 PF14604 | 6.5 | Kd | ChEMBL;BindingDB |
| Q9Y2U5 | MAP3K2 | Homo sapiens | Human | PF00564 PF00069 | 6.5 | Kd | ChEMBL;BindingDB |
| Q9UKE5 | TNIK | Homo sapiens | Human | PF00780 PF00069 | 6.5 | Kd | ChEMBL;BindingDB |
| O95819 | MAP4K4 | Homo sapiens | Human | PF00780 PF00069 | 6.5 | Ki | ChEMBL |
| O75716 | STK16 | Homo sapiens | Human | PF00069 | 6.4 | Kd | ChEMBL;BindingDB |
| P53671 | LIMK2 | Homo sapiens | Human | PF00412 PF00595 PF07714 | 6.4 | Kd | ChEMBL;BindingDB |
| Q9NRP7 | STK36 | Homo sapiens | Human | PF13646 PF00069 | 6.3 | Kd | ChEMBL;BindingDB |
| Q13163 | MAP2K5 | Homo sapiens | Human | PF00564 PF00069 | 6.3 | Kd | ChEMBL;BindingDB |
| P06239 | LCK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.3 | Ki | ChEMBL |
| P45983 | MAPK8 | Homo sapiens | Human | PF00069 | 6.3 | Ki | ChEMBL |
| P15056 | BRAF | Homo sapiens | Human | PF00130 PF07714 PF02196 | 6.3 | Kd | ChEMBL;BindingDB |
| P00519 | ABL1 | Homo sapiens | Human | PF08919 PF07714 PF00017 PF00018 | 6.2 | Kd | ChEMBL;BindingDB |
| O43353 | RIPK2 | Homo sapiens | Human | PF00619 PF07714 | 6.2 | Kd | ChEMBL;BindingDB |
| P45985 | MAP2K4 | Homo sapiens | Human | PF00069 | 6.2 | Kd | ChEMBL;BindingDB |
| Q9BVS4 | RIOK2 | Homo sapiens | Human | PF01163 PF09202 | 6.2 | Kd | ChEMBL;BindingDB |
| P22607 | FGFR3 | Homo sapiens | Human | PF21165 PF07679 PF13927 PF07714 | 6.2 | Kd | ChEMBL;BindingDB |
| P35590 | TIE1 | Homo sapiens | Human | PF00041 PF00047 PF07714 | 6.2 | Kd | ChEMBL;BindingDB |
| P53667 | LIMK1 | Homo sapiens | Human | PF00412 PF00595 PF07714 | 6.1 | Kd | ChEMBL;BindingDB |
| Q16584 | MAP3K11 | Homo sapiens | Human | PF07714 PF14604 | 6.1 | Kd | ChEMBL;BindingDB |
| P42685 | FRK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.1 | Kd | ChEMBL;BindingDB |
| Q92918 | MAP4K1 | Homo sapiens | Human | PF00780 PF00069 | 6.1 | Kd | ChEMBL;BindingDB |
| Q9UQB9 | AURKC | Homo sapiens | Human | PF00069 | 6.1 | Kd | ChEMBL;BindingDB |
| O14965 | AURKA | Homo sapiens | Human | PF00069 | 6.1 | Kd | ChEMBL |
| Q9Y616 | IRAK3 | Homo sapiens | Human | PF00531 PF00069 | 6.1 | Kd | ChEMBL;BindingDB |
| P36888 | FLT3 | Homo sapiens | Human | PF00047 PF07714 | 6.1 | Kd | ChEMBL;BindingDB |
| P04049 | RAF1 | Homo sapiens | Human | PF00130 PF07714 PF02196 | 6.0 | Kd | ChEMBL;BindingDB |
| P07948 | LYN | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.0 | Kd | ChEMBL;BindingDB |
| P08922 | ROS1 | Homo sapiens | Human | PF00041 PF07714 | 6.0 | Kd | ChEMBL;BindingDB |
| P22303 | ACHE | Homo sapiens | Human | PF08674 PF00135 | 6.0 | IC50 | ChEMBL;BindingDB |
| Q56UN5 | MAP3K19 | Homo sapiens | Human | PF00069 | 6.0 | Kd | ChEMBL;BindingDB |
| Q9UBF8 | PI4KB | Homo sapiens | Human | PF00454 PF21245 | 6.0 | Kd | ChEMBL;BindingDB |
| P51955 | NEK2 | Homo sapiens | Human | PF00069 | 6.0 | Kd | ChEMBL;BindingDB |
| Q13470 | TNK1 | Homo sapiens | Human | PF07714 PF22931 | 6.0 | Kd | ChEMBL;BindingDB |
| O00238 | BMPR1B | Homo sapiens | Human | PF01064 PF07714 PF08515 | 6.0 | Kd | ChEMBL;BindingDB |
| P62343 | CDPK1 | Plasmodium falciparum (isolate K1 / Thailand) | Pathogen | PF13499 PF00069 | 6.4 | Kd | BindingDB |
DrugBank Target Actions (20)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P08684 | CYP3A4 | Cytochrome P450 3A4 | inhibitor | enzymes |
| P10632 | CYP2C8 | Cytochrome P450 2C8 | inhibitor | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | inhibitor | enzymes |
| P05177 | CYP1A2 | Cytochrome P450 1A2 | substrate | enzymes |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | substrate | enzymes |
| P10632 | CYP2C8 | Cytochrome P450 2C8 | substrate | enzymes |
| P05230 | FGF1 | Fibroblast growth factor 1 | inhibitor | targets |
| P09619 | PDGFRB | Platelet-derived growth factor receptor beta | inhibitor | targets |
| P10721 | KIT | Mast/stem cell growth factor receptor Kit | inhibitor | targets |
| P16234 | PDGFRA | Platelet-derived growth factor receptor alpha | inhibitor | targets |
| P17948 | FLT1 | Vascular endothelial growth factor receptor 1 | inhibitor | targets |
| P22607 | FGFR3 | Fibroblast growth factor receptor 3 | inhibitor | targets |
| P35916 | FLT4 | Vascular endothelial growth factor receptor 3 | inhibitor | targets |
| P35968 | KDR | Vascular endothelial growth factor receptor 2 | inhibitor | targets |
| Q08881 | ITK | Tyrosine-protein kinase ITK/TSK | inhibitor | targets |
| Q9UQQ2 | Q9UQQ2 | SH2B adapter protein 3 | inhibitor | targets |
| P22309 | UGT1A1 | UDP-glucuronosyltransferase 1A1 | inhibitor | transporters |
| Q9Y6L6 | SLCO1B1 | Solute carrier organic anion transporter family member 1B1 | inhibitor | transporters |
| P08183 | ABCB1 | ATP-dependent translocase ABCB1 | substrate | transporters |
| Q9UNQ0 | ABCG2 | Broad substrate specificity ATP-binding cassette transporter ABCG2 | substrate | transporters |