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A3 receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 21

Nomenclature: A3 receptor

Family: Adenosine receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 318 1p13.2 ADORA3 adenosine A3 receptor 1,68,78,81
Mouse 7 319 3 46.45 cM Adora3 adenosine A3 receptor 109
Rat 7 320 2q34 Adora3 adenosine A3 receptor 113
Previous and Unofficial Names Click here for help
Adenosine receptor A3 | TGPCR1 | A3AR | ARA3
Database Links Click here for help
Specialist databases
GPCRdb aa3r_human (Hs), aa3r_mouse (Mm), aa3r_rat (Rn)
Other databases
Alphafold
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
adenosine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]AB-MECA Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.0 – 9.1 pKd 74,97
pKd 9.0 – 9.1 (Kd 1x10-9 – 6x10-10 M) [74,97]
[3H]HEMADO Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.0 pKd 55
pKd 9.0 [55]
[125I]AB-MECA Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.9 pKd 73
pKd 8.9 [73]
[3H]NECA Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 7.9 – 8.2 pKd 26,56
pKd 7.9 – 8.2 [26,56]
[125I]APNEA Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 7.8 pKd 113
pKd 7.8 [113]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Mm Agonist 9.7 pKi 61
pKi 9.7 (Ki 1.8x10-10 M) [61]
MRS3558 Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.5 pKi 46
pKi 9.5 (Ki 2.9x10-10 M) [46]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Rn Agonist 9.5 pKi 61
pKi 9.5 (Ki 3.3x10-10 M) [61]
(R,S)-PHPNECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.4 pKi 101
pKi 9.4 [101]
2-phenylethylyl-adenosine derivative Small molecule or natural product Hs Agonist 9.4 pKi 100
pKi 9.4 (Ki 4.4x10-10 M) [100]
MRS3558 Small molecule or natural product Click here for species-specific activity table Rn Agonist 9.0 pKi 61
pKi 9.0 (Ki 1x10-9 M) [61]
HEMADO Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.0 pKi 55,101
pKi 9.0 (Ki 1.1x10-9 M) [55,101]
piclidenoson Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 8.7 – 9.2 pKi 26,32,56,97
pKi 8.7 – 9.2 [26,32,56,97]
MRS3558 Small molecule or natural product Click here for species-specific activity table Mm Agonist 8.8 pKi 61
pKi 8.8 (Ki 1.49x10-9 M) [61]
MRS5151 Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.6 pKi 66
pKi 8.6 (Ki 2.38x10-9 M) [66]
compound 6c [PMID: 34435786] Small molecule or natural product Hs Agonist 8.6 pKi 59
pKi 8.6 (Ki 2.4x10-9 M) [59]
2-hexynyl-NECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 pKi 101
pKi 8.6 [101]
MRS5698 Small molecule or natural product Hs Agonist 8.5 pKi 90
pKi 8.5 [90]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 – 8.9 pKi 10,47,52
pKi 8.0 – 8.9 [10,47,52]
CP608,039 Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.2 pKi 91
pKi 8.2 (Ki 5.8x10-9 M) [91]
PENECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 101
pKi 8.2 [101]
I-ABA Small molecule or natural product Hs Full agonist 8.0 pKi 81
pKi 8.0 [81]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 97
pKi 8.0 [97]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.5 – 8.4 pKi 9,33,47,81,97,104
pKi 7.5 – 8.4 [9,33,47,81,97,104]
AB-MECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pKi 56,97
pKi 7.7 [56,97]
MRS5151 Small molecule or natural product Click here for species-specific activity table Mm Agonist 7.6 pKi 66
pKi 7.6 (Ki 2.44x10-8 M) [66]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 – 8.1 pKi 33,47,56,81,97
pKi 7.1 – 8.1 [33,47,56,81,97]
CCPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 46,56
pKi 7.4 [46,56]
apadenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 46
pKi 7.3 (Ki 4.5x10-8 M) [46]
cyclopentyladenosine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.0 – 7.4 pKi 33,46,56,81
pKi 7.0 – 7.4 [33,46,56,81]
(S)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 – 7.4 pKi 56,81,97
pKi 6.3 – 7.4 [56,81,97]
MPC-MECA Small molecule or natural product Hs Full agonist 6.8 pKi 97
pKi 6.8 [97]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.6 – 6.9 pKi 64,73
pKi 6.6 – 6.9 [64,73]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.8 pKi 92
pKi 6.8 (Ki 1.76x10-7 M) [92]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 – 6.8 pKi 16,73
pKi 6.6 – 6.8 [16,73]
CCPA Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.6 pKi 61
pKi 6.6 (Ki 2.37x10-7 M) [61]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.0 – 7.2 pKi 9,33,46,56,97
pKi 6.0 – 7.2 [9,33,46,56,97]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 6.5 pKi 29-30,104
pKi 6.5 (Ki 2.9x10-7 M) [29-30,104]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Agonist 6.2 pKi 61
pKi 6.2 (Ki 5.84x10-7 M) [61]
TCPA Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 6
pKi 6.2 (Ki 6x10-7 M) [6]
binodenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.0 pKi 46
pKi 6.0 (Ki 9.03x10-7 M) [46]
GS9667 Small molecule or natural product Click here for species-specific activity table Hs Agonist <6.0 pKi 22
pKi <6.0 (Ki >1x10-6 M) [22]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.0 pKi 79
pKi 6.0 (Ki 1.025x10-6 M) [79]
2-chloroadenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 5.7 pKi 92
pKi 5.7 (Ki 1.89x10-6 M) [92]
2'-Me-CCPA Small molecule or natural product Rn Agonist 5.3 pKi 28
pKi 5.3 (Ki 5x10-6 M) [28]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Agonist 5.2 pKi 104
pKi 5.2 (Ki 6.5x10-6 M) [104]
BAY 60-6583 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist <5.0 pKi 57
pKi <5.0 (Ki >1x10-5 M) [57]
regadenoson Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]MRE 3008F20 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKd 4,97
pKd 9.1 [4,97]
PSB-11 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKd 69
pKd 8.3 (Kd 4.9x10-9 M) [69]
[3H]PSB-11 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 pKd 69
pKd 8.3 [69]
KF26777 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.7 pKi 80
pKi 9.7 (Ki 2x10-10 M) [80]
PSB-10 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKi 71
pKi 9.4 (Ki 4.41x10-10 M) [71]
MRE 3010F20 Small molecule or natural product Hs Antagonist 9.3 pKi 97
pKi 9.3 [97]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.5 pKi 46,96-97
pKi 9.0 – 9.5 [46,96-97]
MRS1220 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.2 pKi 47,54,87,107
pKi 8.2 – 9.2 (Ki 6.31x10-9 – 6.3x10-10 M) [47,54,87,107]
PSB-11 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 75
pKi 8.6 (Ki 2.34x10-9 M) [75]
MRS1177 Small molecule or natural product Hs Antagonist 8.5 pKi 54
pKi 8.5 [54]
VUF5574 Small molecule or natural product Hs Antagonist 8.4 pKi 94
pKi 8.4 (Ki 4.03x10-9 M) [94]
MRS1186 Small molecule or natural product Hs Antagonist 8.1 pKi 54
pKi 8.1 [54]
MRS1505 Small molecule or natural product Hs Antagonist 8.1 pKi 60
pKi 8.1 [60]
LUF7602 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.0 pKi 106
pKi 8.0 (Ki 1x10-8 M) [106]
Description: Displacement of [3H]PSB-11 binding from the hA3AR (in membranes from stably transfected CHO cells) following preincubation for 4 h,
LJ-4517 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 pKi 85
pKi 7.8 (Ki 1.56x10-8 M) [85]
VUF8504 Small molecule or natural product Hs Antagonist 7.8 pKi 93
pKi 7.8 [93]
xanthine amine congener Small molecule or natural product Ligand has a PDB structure Rn Antagonist 7.7 pKi 73
pKi 7.7 [73]
I-ABOPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 81
pKi 7.7 [81]
MRS1476 Small molecule or natural product Hs Antagonist 7.7 pKi 60
pKi 7.7 [60]
MRS1523 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 60
pKi 7.7 (Ki 1.99x10-8 M) [60]
MRS1191 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 47-48,61
pKi 7.5 [47-48,61]
MRS1486 Small molecule or natural product Hs Antagonist 7.5 pKi 60
pKi 7.5 [60]
CGS 15943 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.9 pKi 54,56,74,97
pKi 7.0 – 7.9 [54,56,74,97]
BW-A1433 Small molecule or natural product Rn Antagonist 7.4 pKi 73
pKi 7.4 [73]
BW-A1433 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.3 pKi 81
pKi 7.3 [81]
xanthine amine congener Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.4 pKi 56,81,97
pKi 7.0 – 7.4 [56,81,97]
MRS1097 Small molecule or natural product Hs Antagonist 7.0 pKi 47,95
pKi 7.0 [47,95]
MRS1523 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.9 pKi 61
pKi 6.9 (Ki 1.13x10-7 M) [61]
VUF8507 Small molecule or natural product Hs Antagonist 6.7 pKi 93
pKi 6.7 [93]
derenofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 49
pKi 6.7 (Ki 2x10-7 M) [49]
MRS1042 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 50
pKi 6.5 [50]
MRS1041 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 50
pKi 6.4 [50]
MRS1754 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 53
pKi 6.2 (Ki 5.7x10-7 M) [53]
MRS1067 Small molecule or natural product Hs Antagonist 6.2 pKi 47,50
pKi 6.2 [47,50]
LUF5981 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 12
pKi 6.2 (Ki 6.37x10-7 M) [12]
MRS1523 Small molecule or natural product Click here for species-specific activity table Mm Antagonist 6.1 pKi 61
pKi 6.1 (Ki 7.31x10-7 M) [61]
ZM-241385 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.1 pKi 46
pKi 6.1 (Ki 7.43x10-7 M) [46]
MRS1093 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 50
pKi 6.1 [50]
MRS1088 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 50
pKi 6.1 [50]
DPCPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 – 6.6 pKi 2,39,56,81,97,102
pKi 5.4 – 6.6 (Ki 3.96x10-6 – 2.43x10-7 M) [2,39,56,81,97,102]
MRE 2029F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
vipadenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 6.0 pKi 35
pKi 6.0 (Ki 1.005x10-6 M) [35]
ST-1535 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 67
pKi <6.0 (Ki >1x10-6 M) [67]
preladenant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <6.0 pKi 70
pKi <6.0 (Ki >1x10-6 M) [70]
ATL802 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 53
pKi <6.0 (Ki >1x10-6 M) [53]
DPCPX Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.4 – 7.6 pKi 2,73,102
pKi 4.4 – 7.6 [2,73,102]
LAS38096 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 20,99
pKi 6.0 (Ki 1.043x10-6 M) [20,99]
CVT-6883 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 21
pKi 6.0 (Ki 1.07x10-6 M) [21]
SCH 58261 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 46
pKi 5.9 (Ki 1.2x10-6 M) [46]
MRS928 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 50
pKi 5.9 [50]
MRS1191 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.8 pKi 60-61
pKi 5.8 [60-61]
dexniguldipine Small molecule or natural product Hs Antagonist 5.7 pKi 95
pKi 5.7 [95]
PSB36 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 102
pKi 5.6 (Ki 2.3x10-6 M) [102]
galangin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.5 pKi 50
pKi 5.5 [50]
sakuranetin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.5 pKi 50
pKi 5.5 [50]
nicardipine Small molecule or natural product Approved drug Hs Antagonist 5.5 pKi 95
pKi 5.5 [95]
rolofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 pKi 51
pKi 5.4 (Ki 4.39x10-6 M) [51]
istradefylline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.3 pKi 31
pKi 5.3 (Ki 4.47x10-6 M) [31]
PSB36 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.2 pKi 102
pKi 5.2 (Ki 6.5x10-6 M) [102]
SCH442416 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
PSB603 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB1115 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <5.0 pKi 39
pKi <5.0 (Ki >1x10-5 M) [39]
tonapofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 51
pKi <5.0 (Ki >1x10-5 M) [51]
FK-453 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 pKi 46
pKi 5.0 (Ki 1x10-5 M) [46]
CSC Small molecule or natural product Click here for species-specific activity table Rn Antagonist <5.0 pKi 92
pKi <5.0 (Ki >1x10-5 M) [92]
MSX-2 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 83
pKi <5.0 (Ki >1x10-5 M) [83]
ATL802 Small molecule or natural product Click here for species-specific activity table