Molecule Details
InChIKeyYNNUSGIPVFPVBX-NHCUHLMSSA-N
Compound NameClemastine
Canonical SMILESCN1CCC[C@@H]1CCO[C@](C)(c1ccccc1)c1ccc(Cl)cc1
Clinical Status Clinical Multi-Target
Targets (Human+Pathogen)24
Pfam Stratification Cross-Family
Avg pChEMBL7.29
SourceChEMBL;BindingDB;TTD_MultiTarget
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00283
Drug NameClemastine
CAS Number15686-51-8
Groups approved investigational
ATC Codes D04AA14 R06AA54 R06AA04
DescriptionAn ethanolamine-derivative, first generation histamine H1 antagonist used in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.

Categories: Aminoalkyl Ethers Anti-Allergic Agents Antihistamines for Systemic Use Antihistamines for Topical Use Antipruritics Antipruritics, Incl. Antihistamines, Anesthetics, Etc. Central Nervous System Depressants Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (strength unknown) Cytochrome P-450 Enzyme Inhibitors Dermatologicals Highest Risk QTc-Prolonging Agents Histamine Agents Histamine Antagonists Histamine H1 Antagonists Neurotransmitter Agents Pyrrolidines QTc Prolonging Agents
Cross-references: BindingDB: 94606 ChEBI: 3738 CHEMBL1626 ChemSpider: 25129 Drugs Product Database (DPD): 11240 C06913 D03535 PharmGKB: PA164776997 PubChem:26987 PubChem:46506492 RxCUI: 2578 Therapeutic Targets Database: DAP000322 Wikipedia: Clemastine ZINC: ZINC000000402830
Target Activities (24)
Target Gene Organism Category Pfam pChEMBL Type Source
P35367 HRH1 Homo sapiens Human PF00001 9.8 IC50 ChEMBL
P35462 DRD3 Homo sapiens Human PF00001 8.4 IC50 ChEMBL
Q99720 SIGMAR1 Homo sapiens Human PF04622 7.9 Ki ChEMBL;BindingDB
P08912 CHRM5 Homo sapiens Human PF00001 7.8 Ki ChEMBL;BindingDB
P35348 ADRA1A Homo sapiens Human PF00001 7.8 pIC50 TTD_MultiTarget
P28223 HTR2A Homo sapiens Human PF00001 7.8 IC50 ChEMBL
P11229 CHRM1 Homo sapiens Human PF00001 7.7 Ki ChEMBL;BindingDB
P25100 ADRA1D Homo sapiens Human PF00001 7.7 IC50 ChEMBL
Q5BJF2 TMEM97 Homo sapiens Human PF05241 7.6 Ki ChEMBL;BindingDB
P41595 HTR2B Homo sapiens Human PF00001 7.5 IC50 ChEMBL
P08173 CHRM4 Homo sapiens Human PF00001 7.5 Ki ChEMBL;BindingDB
P20309 CHRM3 Homo sapiens Human PF00001 7.3 Ki ChEMBL;BindingDB
P50406 HTR6 Homo sapiens Human PF00001 7.3 IC50 ChEMBL
P28335 HTR2C Homo sapiens Human PF00001 7.1 IC50 ChEMBL
P14416 DRD2 Homo sapiens Human PF00001 7.1 IC50 ChEMBL
P08172 CHRM2 Homo sapiens Human PF00001 6.9 Ki ChEMBL;BindingDB
P18825 ADRA2C Homo sapiens Human PF00001 6.8 Ki ChEMBL;BindingDB
P08913 ADRA2A Homo sapiens Human PF00001 6.8 Ki ChEMBL;BindingDB
Q12809 KCNH2 Homo sapiens Human PF00027 PF00520 PF13426 6.6 Ki ChEMBL;BindingDB
P25021 HRH2 Homo sapiens Human PF00001 6.4 IC50 ChEMBL
P18089 ADRA2B Homo sapiens Human PF00001 6.4 Ki ChEMBL;BindingDB
P33261 CYP2C19 Homo sapiens Human PF00067 6.2 IC50 ChEMBL
Q01959 SLC6A3 Homo sapiens Human PF00209 6.2 IC50 ChEMBL
P21728 DRD1 Homo sapiens Human PF00001 6.1 Ki ChEMBL
DrugBank Target Actions (2)
Target Gene Target Name Action Type
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P35367 HRH1 Histamine H1 receptor antagonist targets