Molecule Details
InChIKeyZQDWXGKKHFNSQK-UHFFFAOYSA-N
Compound NameHydroxyzine
Canonical SMILESOCCOCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL7.47
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00557
Drug NameHydroxyzine
CAS Number68-88-2
Groups approved investigational
ATC Codes N05BB01 N05BB51
DescriptionHydroxyzine is a first-generation histamine H<sub>1</sub>-receptor antagonist of the dephenylmethane and piperazine classes that exhibits sedative, anxiolytic, and antiemetic properties.[A1257,A187589] It was first developed in 1955,[A189726] and has since remained a relatively common treatment for ...

Categories: Anti-Anxiety Agents Antipruritics Central Nervous System Depressants Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (strength unknown) Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A5 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Dermatologicals Diphenylmethane Derivatives Histamine Agents Histamine Antagonists Histamine H1 Antagonists Histamine Receptor Antagonists Miscellaneous Anxiolytics Sedatives and Hypnotics Nervous System Neurotransmitter Agents P-glycoprotein substrates Piperazines Potential QTc-Prolonging Agents Psycholeptics QTc Prolonging Agents
Cross-references: BindingDB: 22875 ChEBI: 5818 CHEMBL896 ChemSpider: 3531 Drugs Product Database (DPD): 8008 C07045 D08054 PharmGKB: PA449943 PubChem:3658 PubChem:46508556 RxCUI: 5553 Therapeutic Targets Database: DAP000324 Wikipedia: Hydroxyzine
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P35367 HRH1 Homo sapiens Human PF00001 8.7 Ki ChEMBL;BindingDB
P28223 HTR2A Homo sapiens Human PF00001 7.3 Ki ChEMBL;BindingDB
P14416 DRD2 Homo sapiens Human PF00001 6.4 Ki ChEMBL;BindingDB
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P02768 ALB Albumin regulator carriers
P02768 ALB Albumin substrate carriers
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P20815 CYP3A5 Cytochrome P450 3A5 substrate enzymes
Q12809 KCNH2 Voltage-gated inwardly rectifying potassium channel KCNH2 inhibitor targets
P35367 HRH1 Histamine H1 receptor inverse agonist targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters