Molecule Details
InChIKeyFWFGIHPGRQZWIW-SQNIBIBYSA-N
Compound NameTosedostat
Canonical SMILESCC(C)C[C@@H](C(=O)N[C@H](C(=O)OC1CCCC1)c1ccccc1)[C@H](O)C(=O)NO
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)6
Pfam Stratification Cross-Family
Avg pChEMBL7.0
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB11781
Drug NameTosedostat
CAS Number238750-77-1
Groups investigational
ATC Codes nan
DescriptionTosedostat has been used in trials studying the treatment and supportive care of AML, Leukemia, Pancreas Cancer, Multiple Myeloma, and Pancreatic Cancer, among others. Tosedostat is an inhibitor of the M1 family of aminopeptidases, in particular PuSA, and LTA4 hydrolase. It has demonstrated anti-tum...

Categories: Amines Amino Acids Amino Acids, Peptides, and Proteins Enzyme Inhibitors Hydroxy Acids Hydroxylamines
Cross-references: ChEBI: 95044 CHEMBL2103847 ChemSpider: 24606030 PubChem:15547703 PubChem:347828131 ZINC: ZINC000013914293
Target Activities (6)
Target Gene Organism Category Pfam pChEMBL Type Source
P28838 LAP3 Homo sapiens Human PF00883 PF02789 8.3 IC50 ChEMBL
P09960 LTA4H Homo sapiens Human PF09127 PF01433 PF17900 8.1 IC50 ChEMBL
P08253 MMP2 Homo sapiens Human PF00040 PF00045 PF00413 6.7 IC50 ChEMBL;BindingDB
P55786 NPEPPS Homo sapiens Human PF11838 PF01433 PF17900 6.6 IC50 ChEMBL;BindingDB
P15144 ANPEP Homo sapiens Human PF11838 PF01433 PF17900 6.2 IC50 ChEMBL;BindingDB
Q6P179 ERAP2 Homo sapiens Human PF11838 PF01433 PF17900 6.1 IC50 ChEMBL
DrugBank Target Actions (2)
Target Gene Target Name Action Type
P09960 LTA4H Leukotriene A-4 hydrolase binder targets
P55786 NPEPPS Puromycin-sensitive aminopeptidase inhibitor targets