Molecule Details
InChIKeyDRHKJLXJIQTDTD-OAHLLOKOSA-N
Compound NameTamsulosin
Canonical SMILESCCOc1ccccc1OCCN[C@H](C)Cc1ccc(OC)c(S(N)(=O)=O)c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)9
Pfam Stratification Homologous
Avg pChEMBL8.56
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00706
Drug NameTamsulosin
CAS Number106133-20-4
Groups approved investigational
ATC Codes G04CA52 G04CA02 G01AE10 G04CA54 G04CA53
DescriptionTamsulosin is a selective alpha-1A and alpha-1B adrenoceptor antagonist that exerts its greatest effect in the prostate and bladder, where these receptors are most common.[Label] It is indicated for the treatment of signs and symptoms of benign prostatic hypertrophy.[Label] Antagonism of these recep...

Categories: Adrenergic Agents Adrenergic Antagonists Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists Amides Benzene Derivatives Benzenesulfonamides Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Drugs Used in Benign Prostatic Hypertrophy Drugs that are Mainly Renally Excreted Genito Urinary System and Sex Hormones Genitourinary Agents Gynecological Antiinfectives and Antiseptics Hypotensive Agents Neurotransmitter Agents Peripheral alpha-1 blockers Selective Alfa-1-adrenergic Blocking Agents Sulfonamides Sulfones Sulfur Compounds Urological Agents Urologicals
Cross-references: BindingDB: 50060964 ChEBI: 9398 CHEMBL836 ChemSpider: 114457 Drugs Product Database (DPD): 11780 Guide to Pharmacology: 488 IUPHAR: 488 C07124 PDB: JGX PharmGKB: PA451583 PubChem:129211 PubChem:46507763 RxCUI: 77492 Therapeutic Targets Database: DAP000086 Wikipedia: Tamsulosin ZINC: ZINC000001530694
Target Activities (9)
Target Gene Organism Category Pfam pChEMBL Type Source
P25100 ADRA1D Homo sapiens Human PF00001 9.7 Ki ChEMBL;BindingDB
P35348 ADRA1A Homo sapiens Human PF00001 9.7 Ki ChEMBL;BindingDB
P35462 DRD3 Homo sapiens Human PF00001 9.6 Ki ChEMBL;BindingDB
P08908 HTR1A Homo sapiens Human PF00001 9.1 Ki ChEMBL;BindingDB
P35368 ADRA1B Homo sapiens Human PF00001 8.7 Ki ChEMBL;BindingDB
P18825 ADRA2C Homo sapiens Human PF00001 8.1 Ki ChEMBL;BindingDB
P08913 ADRA2A Homo sapiens Human PF00001 7.5 Ki ChEMBL;BindingDB
P14416 DRD2 Homo sapiens Human PF00001 7.5 Ki ChEMBL;BindingDB
P34969 HTR7 Homo sapiens Human PF00001 7.1 Ki ChEMBL;BindingDB
DrugBank Target Actions (6)
Target Gene Target Name Action Type
P02763 P02763 Alpha-1-acid glycoprotein 1 binder carriers
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P25100 ADRA1D Alpha-1D adrenergic receptor antagonist targets
P35348 ADRA1A Alpha-1A adrenergic receptor antagonist targets
P35368 ADRA1B Alpha-1B adrenergic receptor antagonist targets