ChEMBL logo


ChEMBL Statistics
  Loading Statistics...

Target Report Card

Target Name and Classification

Target ID CHEMBL226
Preferred Name Adenosine A1 receptor
Synonyms ADORA1 | Adenosine receptor A1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > nucleotide-like receptor (family a gpcr) > adenosine receptor

Target Components

Component Description Relationship Accession
Adenosine receptor A1 SINGLE PROTEIN P30542

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111329 Adenosine receptor PROTEIN FAMILY
CHEMBL3885512 Adenosine receptor A1/Alpha-2A adrenergic receptor PROTEIN COMPLEX
CHEMBL2096679 Adenosine receptors; A1 & A2 SELECTIVITY GROUP
CHEMBL2095195 Adenosine receptors; A1 & A3 SELECTIVITY GROUP
CHEMBL2096908 Adenosine receptors; A1 & A2b SELECTIVITY GROUP
CHEMBL2096982 Adenosine receptors; A1 & A2a SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL52333 ROLOFYLLINE Adenosine A1 receptor antagonist 3 PubMed PubMed
CHEMBL414157 TONAPOFYLLINE Adenosine A1 receptor antagonist 3 PubMed PubMed
CHEMBL3545407 TRABODENOSON Adenosine A1 receptor agonist 3 Other PubMed
CHEMBL392149 TECADENOSON Adenosine A1 receptor agonist 2 PubMed PubMed PubMed
CHEMBL592435 DERENOFYLLINE Adenosine A1 receptor antagonist 2 PubMed PubMed
CHEMBL2107371 SELODENOSON Adenosine A1 receptor agonist 2 PubMed
CHEMBL3235279 CAPADENOSON Adenosine A1 receptor partial agonist 2 PubMed PubMed
CHEMBL3545162 PBF-680 Adenosine A1 receptor antagonist 2 Other
CHEMBL3545163 AMP579 Adenosine A1 receptor agonist 2 PubMed
CHEMBL3545223 GW493838 Adenosine A1 receptor agonist 2
CHEMBL3545405 BAY1067197 Adenosine A1 receptor agonist 2 Other
CHEMBL3989819 NAXIFYLLINE Adenosine A1 receptor antagonist 2 PubMed
CHEMBL440115 FK453 Adenosine A1 receptor antagonist 1 DOI PubMed
CHEMBL3545011 GS-9667 Adenosine A1 receptor partial agonist 1 PubMed PubMed PubMed
CHEMBL3545331 RPR749 Adenosine A1 receptor agonist 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000163485
Ensembl ENSG00000163485
GO Cellular Component GO:0005783 (endoplasmic reticulum)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0012505 (endomembrane system)
GO:0014069 (postsynaptic density)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0030425 (dendrite)
GO:0030673 (axolemma)
GO:0032279 (asymmetric synapse)
GO:0042734 (presynaptic membrane)
GO:0043025 (neuronal cell body)
GO:0043195 (terminal bouton)
GO:0043197 (dendritic spine)
GO:0044297 (cell body)
GO:0045202 (synapse)
GO:0045211 (postsynaptic membrane)
GO:0048786 (presynaptic active zone)
GO:0099055 (integral component of postsynaptic membrane)
GO:0099056 (integral component of presynaptic membrane)
GO Molecular Function GO:0001609 (G-protein coupled adenosine receptor activity)
GO:0001664 (G-protein coupled receptor binding)
GO:0001883 (purine nucleoside binding)
GO:0004629 (phospholipase C activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0005515 (protein binding)
GO:0031072 (heat shock protein binding)
GO:0031683 (G-protein beta/gamma-subunit complex binding)
GO:0032795 (heterotrimeric G-protein binding)
GO:0046982 (protein heterodimerization activity)
GO Biological Process GO:0000186 (activation of MAPKK activity)
GO:0001659 (temperature homeostasis)
GO:0001666 (response to hypoxia)
GO:0001973 (adenosine receptor signaling pathway)
GO:0002087 (regulation of respiratory gaseous exchange by neurological system process)
GO:0002674 (negative regulation of acute inflammatory response)
GO:0002686 (negative regulation of leukocyte migration)
GO:0002793 (positive regulation of peptide secretion)
GO:0003093 (regulation of glomerular filtration)
GO:0006612 (protein targeting to membrane)
GO:0006909 (phagocytosis)
GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007193 (adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway)
GO:0007267 (cell-cell signaling)
GO:0007399 (nervous system development)
GO:0008285 (negative regulation of cell proliferation)
GO:0014050 (negative regulation of glutamate secretion)
GO:0016042 (lipid catabolic process)
GO:0032229 (negative regulation of synaptic transmission, GABAergic)
GO:0032244 (positive regulation of nucleoside transport)
GO:0032900 (negative regulation of neurotrophin production)
GO:0035307 (positive regulation of protein dephosphorylation)
GO:0035814 (negative regulation of renal sodium excretion)
GO:0042321 (negative regulation of circadian sleep/wake cycle, sleep)
GO:0042323 (negative regulation of circadian sleep/wake cycle, non-REM sleep)
GO:0043066 (negative regulation of apoptotic process)
GO:0043268 (positive regulation of potassium ion transport)
GO:0045741 (positive regulation of epidermal growth factor-activated receptor activity)
GO:0045776 (negative regulation of blood pressure)
GO:0045777 (positive regulation of blood pressure)
GO:0045822 (negative regulation of heart contraction)
GO:0046888 (negative regulation of hormone secretion)
GO:0048167 (regulation of synaptic plasticity)
GO:0050728 (negative regulation of inflammatory response)
GO:0050890 (cognition)
GO:0050965 (detection of temperature stimulus involved in sensory perception of pain)
GO:0050995 (negative regulation of lipid catabolic process)
GO:0051930 (regulation of sensory perception of pain)
GO:0051967 (negative regulation of synaptic transmission, glutamatergic)
GO:0055117 (regulation of cardiac muscle contraction)
GO:0055118 (negative regulation of cardiac muscle contraction)
GO:0060079 (excitatory postsynaptic potential)
GO:0060087 (relaxation of vascular smooth muscle)
GO:0070256 (negative regulation of mucus secretion)
GO:0097190 (apoptotic signaling pathway)
GO:0097756 (negative regulation of blood vessel diameter)
GO:1900453 (negative regulation of long term synaptic depression)
Wikipedia Adenosine_A1_receptor

Target Cross References - Protein

canSAR P30542
Human Protein Atlas ENSG00000163485
IntAct P30542
Guide to Pharmacology 18
MICAD NBK23601 (Adenosine A1 receptor)
NBK23624 (Adenosine A1 receptor)
Open Targets ENSG00000163485
PharmGKB PA24583
Pharos P30542 (Tclin)
Reactome R-HSA-417973 (Adenosine P1 receptors.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt A6NFY5 A6NGP4 A8K1L3 B3KXQ4 D2CGD0 P30542 Q6FHK3 Q8TAM8

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR001068 (Adeno_A1_rcpt.)
IPR001634 (Adenosn_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure