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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
CHEMBL2111467 Alpha adrenergic receptor (1a and 1d) SELECTIVITY GROUP
CHEMBL2094251 Adrenergic receptor alpha-1 PROTEIN FAMILY
CHEMBL2095203 Adrenergic receptor alpha PROTEIN FAMILY
CHEMBL2331074 Adrenergic receptor PROTEIN FAMILY
CHEMBL2096676 Adrenergic receptors; alpha-1 A & B 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:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005901 (caveola)
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:0005515 (protein binding)
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:0010507 (negative regulation of autophagy)
GO:0010613 (positive regulation of cardiac muscle hypertrophy)
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:0061049 (cell growth involved in cardiac muscle cell development)
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)
GO:1903997 (positive regulation of non-membrane spanning protein tyrosine kinase activity)
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)