Molecule Details
InChIKeyXTTZERNUQAFMOF-QMMMGPOBSA-N
Compound NameLorcaserin
Canonical SMILESC[C@H]1CNCCc2ccc(Cl)cc21
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL7.19
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB04871
Drug NameLorcaserin
CAS Number616202-92-7
Groups approved withdrawn
ATC Codes A08AA11
DescriptionLorcaserin (previously APD-356), a highly selective 5HT2C receptor agonist, is used for the treatment of obesity. It has been shown to reduce body weight and food intake in animal models of obesity, and it is thought that targeting the 5HT2C receptor may alter body weight by regulating satiety. Lorc...

Categories: Alimentary Tract and Metabolism Antidepressive Agents Antiobesity Preparations, Excl. Diet Products Central Nervous System Depressants Centrally Acting Antiobesity Products Cytochrome P-450 CYP1A1 Substrates Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2A6 Substrates Cytochrome P-450 CYP2B6 Substrates Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (moderate) Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Drugs that are Mainly Renally Excreted Heterocyclic Compounds, Fused-Ring Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin 2c Receptor Agonists Serotonin 5-HT2 Receptor Agonists Serotonin 5-HT2C Receptor Agonists Serotonin Agents Serotonin Modulators Serotonin Receptor Agonists
Cross-references: BindingDB: 50161646 ChEBI: 65353 CHEMBL360328 ChemSpider: 9833595 D06613 PDB: T4U PubChem:11658860 PubChem:310264855 RxCUI: 1300701 Wikipedia: Lorcaserin ZINC: ZINC000006733300
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P28335 HTR2C Homo sapiens Human PF00001 7.8 Ki ChEMBL;BindingDB
P28223 HTR2A Homo sapiens Human PF00001 7.0 Ki ChEMBL;BindingDB
P41595 HTR2B Homo sapiens Human PF00001 6.8 Ki ChEMBL;BindingDB
DrugBank Target Actions (10)
Target Gene Target Name Action Type
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P04798 CYP1A1 Cytochrome P450 1A1 substrate enzymes
P05177 CYP1A2 Cytochrome P450 1A2 substrate enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P11509 CYP2A6 Cytochrome P450 2A6 substrate enzymes
P20813 CYP2B6 Cytochrome P450 2B6 substrate enzymes
P33261 CYP2C19 Cytochrome P450 2C19 substrate enzymes
Q01740 Q01740 Flavin-containing monooxygenase 1 substrate enzymes
P28335 HTR2C 5-hydroxytryptamine receptor 2C agonist targets