Molecule Details
InChIKeyFGXWKSZFVQUSTL-UHFFFAOYSA-N
Compound NameDomperidone
Canonical SMILESO=c1[nH]c2ccccc2n1CCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1
Clinical Status Clinical Multi-Target
Targets (Human+Pathogen)10
Pfam Stratification Cross-Family
Avg pChEMBL6.95
SourceChEMBL;BindingDB;TTD_MultiTarget
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB01184
Drug NameDomperidone
CAS Number57808-66-9
Groups approved investigational vet_approved
ATC Codes A03FA03
DescriptionA specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

Categories: Alimentary Tract and Metabolism Antiemetics Autonomic Agents Benzimidazoles Central Nervous System Agents Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2B6 Substrates Cytochrome P-450 CYP2C8 Substrates Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A5 Substrates Cytochrome P-450 CYP3A7 Substrates Cytochrome P-450 Substrates Dopamine Agents Dopamine Antagonists Dopamine D2 Receptor Antagonists Drugs for Functional Gastrointestinal Disorders Gastrointestinal Agents Heterocyclic Compounds, Fused-Ring Highest Risk QTc-Prolonging Agents Neurotransmitter Agents P-glycoprotein substrates Peripheral Nervous System Agents Piperidines Prokinetic Agents Propulsives QTc Prolonging Agents
Cross-references: BindingDB: 50241107 ChEBI: 31515 CHEMBL219916 ChemSpider: 3039 Drugs Product Database (DPD): 1840 Guide to Pharmacology: 965 IUPHAR: 965 D01745 PDB: A1IVJ PharmGKB: PA134711056 PubChem:3151 PubChem:46508314 RxCUI: 3626 Therapeutic Targets Database: DAP001368 Wikipedia: Domperidone ZINC: ZINC000004175569
Target Activities (10)
Target Gene Organism Category Pfam pChEMBL Type Source
P14416 DRD2 Homo sapiens Human PF00001 8.9 Ki ChEMBL;BindingDB
P35462 DRD3 Homo sapiens Human PF00001 8.1 Ki ChEMBL;BindingDB
P28223 HTR2A Homo sapiens Human PF00001 7.7 IC50 ChEMBL
P35367 HRH1 Homo sapiens Human PF00001 6.8 Ki ChEMBL
Q12809 KCNH2 Homo sapiens Human PF00027 PF00520 PF13426 6.8 IC50 ChEMBL;BindingDB
P18825 ADRA2C Homo sapiens Human PF00001 6.4 IC50 ChEMBL
P25100 ADRA1D Homo sapiens Human PF00001 6.3 Ki ChEMBL
P35348 ADRA1A Homo sapiens Human PF00001 6.3 pIC50 TTD_MultiTarget
P28335 HTR2C Homo sapiens Human PF00001 6.2 Ki ChEMBL
P18089 ADRA2B Homo sapiens Human PF00001 6.0 Ki ChEMBL
DrugBank Target Actions (11)
Target Gene Target Name Action Type
P05177 CYP1A2 Cytochrome P450 1A2 substrate enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10632 CYP2C8 Cytochrome P450 2C8 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P20813 CYP2B6 Cytochrome P450 2B6 substrate enzymes
P20815 CYP3A5 Cytochrome P450 3A5 substrate enzymes
P24462 CYP3A7 Cytochrome P450 3A7 substrate enzymes
P14416 DRD2 D(2) dopamine receptor antagonist targets
P35462 DRD3 D(3) dopamine receptor antagonist targets
P28223 HTR2A 5-hydroxytryptamine receptor 2A inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters