Molecule Details
| InChIKey | WJEOLQLKVOPQFV-UHFFFAOYSA-N |
|---|---|
| Compound Name | Masitinib |
| Canonical SMILES | Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nc(-c2cccnc2)cs1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 24 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.09 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB11526 |
|---|---|
| Drug Name | Masitinib |
| CAS Number | 790299-79-5 |
| Groups | investigational vet_approved |
| ATC Codes | L01EX06 |
| Description | Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in dogs. It has been available in Europe since 2009, under the brand name Masivet. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011. |
Categories: Acids, Carbocyclic Amides Antineoplastic Agents Antineoplastic and Immunomodulating Agents Benzene Derivatives Benzoates Protein Kinase Inhibitors Sulfur Compounds
Cross-references: BindingDB: 50355495 ChEBI: 63450 CHEMBL1908391 ChemSpider: 8250179 D10229 PDB: G65 Wikipedia: Masitinib ZINC: ZINC000034177219
Target Activities (24)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P12236 | SLC25A6 | Homo sapiens | Human | PF00153 | 8.2 | Kd | ChEMBL |
| P07333 | CSF1R | Homo sapiens | Human | PF00047 PF25305 PF07714 | 8.1 | Kd | ChEMBL;BindingDB |
| P10721 | KIT | Homo sapiens | Human | PF00047 PF07714 | 8.1 | Kd | ChEMBL;BindingDB |
| P09619 | PDGFRB | Homo sapiens | Human | PF00047 PF13927 PF25305 PF07714 | 8.1 | Kd | ChEMBL;BindingDB |
| Q08345 | DDR1 | Homo sapiens | Human | PF21114 PF00754 PF07714 | 8.1 | Kd | ChEMBL;BindingDB |
| Q15067 | ACOX1 | Homo sapiens | Human | PF01756 PF22924 PF02770 PF14749 | 7.8 | Kd | ChEMBL |
| P00519 | ABL1 | Homo sapiens | Human | PF08919 PF07714 PF00017 PF00018 | 7.6 | Kd | ChEMBL;BindingDB |
| P16234 | PDGFRA | Homo sapiens | Human | PF07679 PF25305 PF07714 | 7.6 | Kd | ChEMBL;BindingDB |
| Q16832 | DDR2 | Homo sapiens | Human | PF21114 PF00754 PF07714 | 7.6 | Kd | ChEMBL;BindingDB |
| P06239 | LCK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 7.5 | Kd | ChEMBL;BindingDB |
| P07948 | LYN | Homo sapiens | Human | PF07714 PF00017 PF00018 | 7.2 | Kd | ChEMBL;BindingDB |
| P11274 | BCR | Homo sapiens | Human | PF09036 PF00168 PF19057 PF00620 PF00621 | 7.1 | Kd | ChEMBL |
| P42685 | FRK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 7.1 | Kd | ChEMBL;BindingDB |
| P42684 | ABL2 | Homo sapiens | Human | PF08919 PF07714 PF00017 PF00018 | 7.0 | Kd | ChEMBL;BindingDB |
| P06241 | FYN | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.8 | Kd | ChEMBL;BindingDB |
| P51451 | BLK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.8 | Kd | ChEMBL;BindingDB |
| P16083 | NQO2 | Homo sapiens | Human | PF02525 | 6.3 | Kd | ChEMBL |
| P07947 | YES1 | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.2 | Kd | ChEMBL;BindingDB |
| P09769 | FGR | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.2 | Kd | ChEMBL;BindingDB |
| P08631 | HCK | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.2 | Kd | ChEMBL;BindingDB |
| Q86V86 | PIM3 | Homo sapiens | Human | PF00069 | 6.1 | Kd | ChEMBL;BindingDB |
| Q9NYL2 | MAP3K20 | Homo sapiens | Human | PF07714 PF07647 | 6.1 | Kd | ChEMBL;BindingDB |
| P00533 | EGFR | Homo sapiens | Human | PF00757 PF14843 PF07714 PF01030 PF21314 | 6.1 | Kd | ChEMBL;BindingDB |
| P12931 | SRC | Homo sapiens | Human | PF07714 PF00017 PF00018 | 6.0 | Kd | ChEMBL;BindingDB |
DrugBank Target Actions (1)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P12931 | SRC | Proto-oncogene tyrosine-protein kinase Src | inhibitor | targets |