Molecule Details
InChIKeyLUBHDINQXIHVLS-UHFFFAOYSA-N
Compound NameTolrestat
Canonical SMILESCOc1ccc2c(C(=S)N(C)CC(=O)O)cccc2c1C(F)(F)F
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL7.02
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB02383
Drug NameTolrestat
CAS Number82964-04-3
Groups approved withdrawn
ATC Codes A10XA01
DescriptionTolrestat (INN) (AY-27773) is an aldose reductase inhibitor which was approved for the control of certain diabetic complications. While it was approved for marketed in several countries, it failed a Phase III trial in the U.S. due to toxicity and never received FDA approval. It was sold under the tr...

Categories: Aldehyde Reductase, antagonists & inhibitors Aldose Reductase Inhibitors Alimentary Tract and Metabolism Drugs Used in Diabetes Enzyme Inhibitors
Cross-references: BindingDB: 16314 ChEBI: 48549 CHEMBL436 ChemSpider: 48194 C01621 D02323 PDB: TOL PubChem:53359 PubChem:46508274 RxCUI: 38386 Therapeutic Targets Database: DNC001455 Wikipedia: Tolrestat ZINC: ZINC000003780343
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P15121 AKR1B1 Homo sapiens Human PF00248 7.6 IC50 ChEMBL;BindingDB
O60218 AKR1B10 Homo sapiens Human PF00248 7.3 IC50 ChEMBL;BindingDB
P14550 AKR1A1 Homo sapiens Human PF00248 6.1 IC50 ChEMBL;BindingDB
DrugBank Target Actions (4)
Target Gene Target Name Action Type
O60218 AKR1B10 Aldo-keto reductase family 1 member B10 binder targets
P14550 AKR1A1 Aldo-keto reductase family 1 member A1 binder targets
Q99720 SIGMAR1 Sigma non-opioid intracellular receptor 1 binder targets
P15121 AKR1B1 Aldo-keto reductase family 1 member B1 inhibitor targets