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Target Report Card

Target Name and Classification

Target ID CHEMBL229
Preferred Name Alpha-1a adrenergic receptor
Synonyms ADRA1A | ADRA1C | Alpha-1A adrenergic receptor | Alpha-1A adrenoceptor | Alpha-1A adrenoreceptor | Alpha-1C adrenergic receptor | Alpha-adrenergic receptor 1c
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > monoamine receptor > adrenergic receptor

Target Components

Component Description Relationship Accession
Alpha-1A adrenergic receptor SINGLE PROTEIN P35348

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2096676 Adrenergic receptors; alpha-1 A & B SELECTIVITY GROUP
CHEMBL2094251 Adrenergic receptor alpha-1 PROTEIN FAMILY
CHEMBL2331074 Adrenergic receptor PROTEIN FAMILY
CHEMBL2095203 Adrenergic receptor alpha PROTEIN FAMILY
CHEMBL2111467 Alpha adrenergic receptor (1a and 1d) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL24778 SILODOSIN Alpha-1a adrenergic receptor antagonist 4 DailyMed
CHEMBL1200695 PHENYLPROPANOLAMINE HYDROCHLORIDE Alpha-1a adrenergic receptor agonist 4 PubMed
CHEMBL1201044 DAPIPRAZOLE HYDROCHLORIDE Alpha-1a adrenergic receptor antagonist 4 PubMed
CHEMBL1201535 PHENYLPROPANOLAMINE POLISTIREX Alpha-1a adrenergic receptor agonist 4 PubMed
CHEMBL257978 DABUZALGRON Alpha-1a adrenergic receptor partial agonist 2 PubMed
CHEMBL2104986 TEDATIOXETINE Alpha-1a adrenergic receptor antagonist 2 Other Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000120907
Ensembl ENSG00000120907
GO Cellular Component GO:0005634 (nucleus)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030018 (Z disc)
GO:0030315 (T-tubule)
GO:0031965 (nuclear membrane)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004935 (adrenergic receptor activity)
GO:0004937 (alpha1-adrenergic receptor activity)
GO:0046982 (protein heterodimerization activity)
GO Biological Process GO:0001985 (negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressure)
GO:0001994 (norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure)
GO:0001996 (positive regulation of heart rate by epinephrine-norepinephrine)
GO:0001997 (positive regulation of the force of heart contraction by epinephrine-norepinephrine)
GO:0003084 (positive regulation of systemic arterial blood pressure)
GO:0006915 (apoptotic process)
GO:0006937 (regulation of muscle contraction)
GO:0006939 (smooth muscle contraction)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007202 (activation of phospholipase C activity)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007267 (cell-cell signaling)
GO:0007512 (adult heart development)
GO:0007568 (aging)
GO:0008285 (negative regulation of cell proliferation)
GO:0009725 (response to hormone)
GO:0010460 (positive regulation of heart rate)
GO:0016049 (cell growth)
GO:0019229 (regulation of vasoconstriction)
GO:0032230 (positive regulation of synaptic transmission, GABAergic)
GO:0035024 (negative regulation of Rho protein signal transduction)
GO:0035265 (organ growth)
GO:0035556 (intracellular signal transduction)
GO:0042493 (response to drug)
GO:0043410 (positive regulation of MAPK cascade)
GO:0045760 (positive regulation of action potential)
GO:0045907 (positive regulation of vasoconstriction)
GO:0045987 (positive regulation of smooth muscle contraction)
GO:0055117 (regulation of cardiac muscle contraction)
GO:0060073 (micturition)
GO:0060402 (calcium ion transport into cytosol)
GO:0060452 (positive regulation of cardiac muscle contraction)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071880 (adenylate cyclase-activating adrenergic receptor signaling pathway)
GO:0090037 (positive regulation of protein kinase C signaling)
GO:0097195 (pilomotor reflex)
Wikipedia Alpha-1A_adrenergic_receptor

Target Cross References - Protein

canSAR P35348
Human Protein Atlas ENSG00000120907
IntAct P35348
Guide to Pharmacology 22
Open Targets ENSG00000120907
PharmGKB PA34
Pharos P35348 (Tclin)
Reactome R-HSA-390696 (Adrenoceptors.)
R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-416482 (G alpha (12/13) signalling events.)
UniProt A8K0I3 B0ZBD1 B0ZBD2 B0ZBD4 B0ZBD5 B0ZBD6 B0ZBD8 B0ZBD9 O60451 P35348 Q13675 Q13729 Q4VBM7 Q6RUJ4 Q6RUJ5 Q6RUJ7 Q6RUJ8 Q6RUJ9 Q96RE8 Q9UD63 Q9UD67

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR001004 (ADRA1A_rcpt.)
IPR002233 (ADR_fam.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)