Molecule Details
InChIKeyJQSHBVHOMNKWFT-UHFFFAOYSA-N
Compound Name5,8,14-Triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
Canonical SMILESc1cnc2cc3c(cc2n1)C1CNCC3C1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL8.21
SourceBindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB01273
Drug NameVarenicline
CAS Number249296-44-4
Groups approved investigational
ATC Codes S01XA28 N07BA03
DescriptionVarenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 ...

Categories: Benzazepines Cholinergic Agents Cholinergic Agonists Cholinergic Receptor Agonist Drugs Used in Addictive Disorders Drugs Used in Nicotine Dependence Drugs that are Mainly Renally Excreted Heterocyclic Compounds, Fused-Ring Miscellaneous Autonomic Drugs Nervous System Neurotransmitter Agents Nicotinic Agonists OCT2 Inhibitors OCT2 Substrates Ophthalmologicals Partial Cholinergic Nicotinic Agonist Partial Cholinergic Nicotinic Agonists Quinoxalines Sensory Organs Smoking Cessation Agents
Cross-references: BindingDB: 50166908 ChEBI: 84500 CHEMBL1396 ChemSpider: 148958 Drugs Product Database (DPD): 20097 PDB: QMR PharmGKB: PA164781343 PubChem:5310966 PubChem:46505502 RxCUI: 591622 Therapeutic Targets Database: DAP001535 Wikipedia: Varenicline ZINC: ZINC000001481833
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P17787 CHRNB2 Homo sapiens Human PF02931 PF02932 9.3 Ki BindingDB
P43681 CHRNA4 Homo sapiens Human PF02931 PF02932 8.4 Ki BindingDB
P36544 CHRNA7 Homo sapiens Human PF02931 PF02932 6.9 Ki BindingDB
DrugBank Target Actions (7)
Target Gene Target Name Action Type
P36544 CHRNA7 Neuronal acetylcholine receptor subunit alpha-7 agonist targets
P17787 CHRNB2 Neuronal acetylcholine receptor subunit beta-2 partial agonist targets
P32297 CHRNA3 Neuronal acetylcholine receptor subunit alpha-3 partial agonist targets
P43681 CHRNA4 Neuronal acetylcholine receptor subunit alpha-4 partial agonist targets
Q15825 CHRNA6 Neuronal acetylcholine receptor subunit alpha-6 partial agonist targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
O15244 SLC22A2 Solute carrier family 22 member 2 substrate transporters