Molecule Details
InChIKeyOOGJQPCLVADCPB-HXUWFJFHSA-N
Compound NameTolterodine
Canonical SMILESCc1ccc(O)c([C@H](CCN(C(C)C)C(C)C)c2ccccc2)c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)9
Pfam Stratification Cross-Family
Avg pChEMBL7.84
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB01036
Drug NameTolterodine
CAS Number124937-51-5
Groups approved investigational
ATC Codes G04BD07
DescriptionTolterodine is an antimuscarinic drug that is used to treat urinary incontinence. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors.

Categories: Agents producing tachycardia Alcohols Amines Amino Alcohols Anticholinergic Agents Benzene Derivatives Benzhydryl Compounds Cholinergic Agents Cresols Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2C9 Substrates Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Drugs for Urinary Frequency and Incontinence Drugs that are Mainly Renally Excreted Genito Urinary System and Sex Hormones Genitourinary Agents Genitourinary Smooth Muscle Relaxants Muscarinic Antagonists Neurotransmitter Agents Phenols Potential QTc-Prolonging Agents Propanolamines Propanols QTc Prolonging Agents Urological Agents Urologicals
Cross-references: BindingDB: 50165008 ChEBI: 9622 CHEMBL1382 ChemSpider: 391967 Drugs Product Database (DPD): 20821 C07750 D00646 PharmGKB: PA164746757 PubChem:443879 PubChem:46508059 RxCUI: 119565 Therapeutic Targets Database: DAP000376 Wikipedia: Tolterodine ZINC: ZINC000000968336
Target Activities (9)
Target Gene Organism Category Pfam pChEMBL Type Source
P11229 CHRM1 Homo sapiens Human PF00001 8.8 Ki ChEMBL;BindingDB
P08912 CHRM5 Homo sapiens Human PF00001 8.7 Ki ChEMBL;BindingDB
P08173 CHRM4 Homo sapiens Human PF00001 8.5 Ki ChEMBL;BindingDB
P20309 CHRM3 Homo sapiens Human PF00001 8.4 Ki ChEMBL;BindingDB
P08172 CHRM2 Homo sapiens Human PF00001 8.4 Ki ChEMBL;BindingDB
Q12809 KCNH2 Homo sapiens Human PF00027 PF00520 PF13426 7.3 IC50 ChEMBL;BindingDB
P35367 HRH1 Homo sapiens Human PF00001 6.9 Ki ChEMBL
Q5BJF2 TMEM97 Homo sapiens Human PF05241 6.8 Ki ChEMBL
Q99720 SIGMAR1 Homo sapiens Human PF04622 6.7 Ki ChEMBL
DrugBank Target Actions (9)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P11712 CYP2C9 Cytochrome P450 2C9 substrate enzymes
P33261 CYP2C19 Cytochrome P450 2C19 substrate enzymes
P08172 CHRM2 Muscarinic acetylcholine receptor M2 antagonist targets
P08173 CHRM4 Muscarinic acetylcholine receptor M4 antagonist targets
P08912 CHRM5 Muscarinic acetylcholine receptor M5 antagonist targets
P11229 CHRM1 Muscarinic acetylcholine receptor M1 antagonist targets
P20309 CHRM3 Muscarinic acetylcholine receptor M3 antagonist targets