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A2A receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 19

Nomenclature: A2A receptor

Family: Adenosine receptors

Contents:

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 7 412 22q11.23 ADORA2A adenosine A2a receptor 43,72,108
Mouse 7 410 10 C1 Adora2a adenosine A2a receptor 85
Rat 7 410 20p12 Adora2a adenosine A2a receptor 22
Previous and Unofficial Names Click here for help
RDC8 | A2-AR | adenosine receptor A2a
Database Links Click here for help
Specialist databases
GPCRdb aa2ar_human (Hs), aa2ar_mouse (Mm), aa2ar_rat (Rn)
Other databases
Alphafold P29274 (Hs), Q60613 (Mm), P30543 (Rn)
ChEMBL Target CHEMBL251 (Hs), CHEMBL2115 (Mm), CHEMBL302 (Rn)
DrugBank Target P29274 (Hs)
Ensembl Gene ENSG00000128271 (Hs), ENSMUSG00000020178 (Mm), ENSRNOG00000001302 (Rn)
Entrez Gene 135 (Hs), 11540 (Mm), 25369 (Rn)
Human Protein Atlas ENSG00000128271 (Hs)
KEGG Gene hsa:135 (Hs), mmu:11540 (Mm), rno:25369 (Rn)
OMIM 102776 (Hs)
Orphanet ORPHA365126 (Hs)
Pharos P29274 (Hs)
RefSeq Nucleotide NM_000675 (Hs), NM_009630 (Mm), NM_053294 (Rn)
RefSeq Protein NP_000666 (Hs), NP_033760 (Mm), NP_445746 (Rn)
SynPHARM 1495 (in complex with caffeine)
1460 (in complex with CGS 21680)
83711 (in complex with compound 4g [PMID: 22220592])
1467 (in complex with NECA)
1469 (in complex with [3H]CGS 21680)
1470 (in complex with [3H]NECA)
1494 (in complex with [3H]XAC)
82125 (in complex with UK-432,097)
1490 (in complex with xanthine amine congener)
1491 (in complex with ZM-241385)
UniProtKB P29274 (Hs), Q60613 (Mm), P30543 (Rn)
Wikipedia ADORA2A (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Human A2A adenosine receptor bound to an antagonist
PDB Id:  4EIY
Ligand:  ZM-241385
Resolution:  1.8Å
Species:  Human
References:  80
Image of receptor 3D structure from RCSB PDB
Description:  A2A receptor (thermostabilised) bound to its natural ligand adenosine
PDB Id:  2YDO
Ligand:  adenosine   This ligand is endogenous
Resolution:  3.0Å
Species:  Human
References:  73
Image of receptor 3D structure from RCSB PDB
Description:  Thermostabilised human A2A receptor with NECA bound
PDB Id:  2YDV
Ligand:  NECA
Resolution:  2.6Å
Species:  Human
References:  74
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with PSB36
PDB Id:  5N2R
Ligand:  PSB36
Resolution:  2.8Å
Species:  Human
References:  20
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein.
PDB Id:  6GDG
Ligand:  NECA
Resolution:  3.8Å
Species:  Human
References:  47
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
[3H]CGS 21680 Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 7.7 – 7.8 pKd 56,143
⤷ pKd 7.7 – 7.8 (Kd 2.2x10-8 – 1.6x10-8 M) [56,143]
[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 7.7 pKd 67
⤷ pKd 7.7 [67]
apadenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.3 pKi 107
⤷ pKi 9.3 (Ki 5x10-10 M) [107]
(R,S)-PHPNECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.5 pKi 142
⤷ pKi 8.5 [142]
2-hexynyl-NECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 8.3 pKi 32,68,142
⤷ pKi 8.2 – 8.3 [32,68,142]
compound 4g [PMID: 22220592] Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Agonist 8.1 pKi 24
⤷ pKi 8.1 (Ki 7.76x10-9 M) [24]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Agonist 8.0 pKi 82
⤷ pKi 8.0 (Ki 9.7x10-9 M) [82]
UK-432,097 Small molecule or natural product Ligand has a PDB structure Hs Agonist 7.7 – 8.3 pKi 50,148
⤷ pKi 7.7 – 8.3 [50,148]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.9 – 8.7 pKi 14,32,45,63,68,149
⤷ pKi 6.9 – 8.7 [14,32,45,63,68,149]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Agonist 7.7 pKi 79
⤷ pKi 7.7 (Ki 1.9x10-8 M) [79]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.7 – 8.1 pKi 14,32,45,55,63,67-68,101
⤷ pKi 6.7 – 8.1 (Ki 1.99x10-7 – 7.94x10-9 M) [14,32,45,55,63,67-68,101]
2-chloroadenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 7.1 pKi 28
⤷ pKi 7.1 (Ki 7.6x10-8 M) [28]
CV-1808 Small molecule or natural product Hs Full agonist 7.1 pKi 32,68
⤷ pKi 7.1 [32,68]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Agonist 6.8 pKi 149
⤷ pKi 6.8 (Ki 1.5x10-7 M) [149]
2-chloroadenosine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 – 6.8 pKi 63,68
⤷ pKi 6.7 – 6.8 [63,68]
TCPA Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pKi 10
⤷ pKi 6.7 (Ki 2.1x10-7 M) [10]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.7 pKi 28
⤷ pKi 6.7 (Ki 2.2x10-7 M) [28]
binodenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.6 pKi 55
⤷ pKi 6.6 (Ki 2.7x10-7 M) [55]
regadenoson Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 6.5 pKi 55
⤷ pKi 6.5 (Ki 2.9x10-7 M) [55]
adenosine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 6.5 pKi 39-40,149
⤷ pKi 6.5 (Ki 3.1x10-7 M) [39-40,149]
CGS 24012 Small molecule or natural product Hs Full agonist 6.4 pKi 63
⤷ pKi 6.4 [63]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.3 pKi 28
⤷ pKi 6.3 (Ki 4.6x10-7 M) [28]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.3 pKi 79
⤷ pKi 6.3 (Ki 4.7x10-7 M) [79]
PENECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 pKi 142
⤷ pKi 6.2 [142]
cyclopentyladenosine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.1 pKi 45,55,67
⤷ pKi 6.1 [45,55,67]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 – 6.2 pKi 32,45,63,67-68
⤷ pKi 6.0 – 6.2 [32,45,63,67-68]
CCPA Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.0 pKi 79
⤷ pKi 6.0 (Ki 9.5x10-7 M) [79]
cyclopentyladenosine Small molecule or natural product Ligand has a PDB structure Rn Agonist 6.0 pKi 79
⤷ pKi 6.0 (Ki 9.5x10-7 M) [79]
MRS3558 Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.0 pKi 79
⤷ pKi 6.0 (Ki 1.08x10-6 M) [79]
piclidenoson Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 5.6 – 6.3 pKi 55,63,67
⤷ pKi 5.6 – 6.3 [55,63,67]
HEMADO Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.9 pKi 66,142
⤷ pKi 5.9 (Ki 1.2x10-6 M) [66,142]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.9 pKi 32,68
⤷ pKi 5.9 [32,68]
GR79236 Small molecule or natural product Hs Agonist 5.9 pKi 55
⤷ pKi 5.9 (Ki 1.3x10-6 M) [55]
CV-1674 Small molecule or natural product Hs Full agonist 5.8 pKi 68
⤷ pKi 5.8 [68]
tecadenoson Small molecule or natural product Click here for species-specific activity table Pig Agonist 5.6 pKi 55,93
⤷ pKi 5.6 (Ki 2.315x10-6 M) [55,93]
MRS3558 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.6 pKi 55
⤷ pKi 5.6 (Ki 2.33x10-6 M) [55]
CCPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 55,67
⤷ pKi 5.6 [55,67]
metrifudil Small molecule or natural product Hs Full agonist 5.5 pKi 68
⤷ pKi 5.5 [68]
AB-MECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 67
⤷ pKi 5.4 [67]
APNEA Small molecule or natural product Hs Full agonist 5.3 pKi 68
⤷ pKi 5.3 [68]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.3 pKi 55
⤷ pKi 5.3 (Ki 5.36x10-6 M) [55]
(S)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.1 pKi 32,67
⤷ pKi 5.0 – 5.1 [32,67]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Mm Agonist ~5.0 pKi 79
⤷ pKi ~5.0 (Ki ~1x10-5 M) [79]
BAY 60-6583 Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 70
⤷ pKi <5.0 (Ki >1x10-5 M) [70]
GS9667 Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 37
⤷ pKi <5.0 (Ki >1x10-5 M) [37]
MRS5151 Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 88
⤷ pKi <5.0 (Ki >1x10-5 M) [88]
MRS5151 Small molecule or natural product Click here for species-specific activity table Mm Agonist <5.0 pKi 88
⤷ pKi <5.0 (Ki >1x10-5 M) [88]
MRS3558 Small molecule or natural product Click here for species-specific activity table Mm Agonist 5.0 pKi 79
⤷ pKi 5.0 (Ki 1.04x10-5 M) [79]
View species-specific agonist tables
Agonist Comments
The INN-assigned compound evodenoson is an agonist of the A2A receptor but affinity data is not available.
Note that for tecadenoson, there is inconsistency between the two referenced articles (from the same group) as to the species origin of the ADORA2A used to generate the Ki value which is presented as identical in both articles. We have used the earlier paper as precedent, which indicates the use of the porcine receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]ZM-241385 Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 9.2 pKd 106
⤷ pKd 9.2 [106]
[3H]ZM 241385 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.7 – 9.1 pKd 4,44
⤷ pKd 8.7 – 9.1 (Kd 1.8x10-9 – 8x10-10 M) [4,44]
[3H]SCH 58261 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.6 – 9.0 pKd 68,104
⤷ pKd 8.6 – 9.0 [68,104]
[3H]XAC Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 8.0 pKd 63
⤷ pKd 8.0 [63]
SCH442416 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 10.3 pKi 128,132
⤷ pKi 8.4 – 10.3 [128,132]
MRS1093 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.2 pKi 60
⤷ pKi 9.2 [60]
preladenant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.1 pKi 92
⤷ pKi 9.1 (Ki 9x10-10 M) [92]
ZM-241385 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.8 – 9.1 pKi 104
⤷ pKi 8.8 – 9.1 [104]
vipadenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 8.9 pKi 48
⤷ pKi 8.9 (Ki 1.3x10-9 M) [48]
imaradenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 8.8 pKi 12
⤷ pKi 8.8 (Ki 1.7x10-9 M) [12]
Description: Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2AR.
SCH 58261 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 – 9.2 pKi 32,68,104
⤷ pKi 8.3 – 9.2 [32,68,104]
xanthine amine congener Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.4 – 9.0 pKi 32,67
⤷ pKi 8.4 – 9.0 [32,67]
CGS 15943 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.7 – 9.4 pKi 32,63,67,104
⤷ pKi 7.7 – 9.4 [32,63,67,104]
istradefylline Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.4 – 8.7 pKi 113,127
⤷ pKi 8.4 – 8.7 (Ki 4.46x10-9 – 2.2x10-9 M) [113,127]
tozadenant Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 8.3 pKi 29
⤷ pKi 8.3 (Ki 5x10-9 M) [29]
ST-1535 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 89
⤷ pKi 8.2 (Ki 6.6x10-9 M) [89]
MSX-2 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.1 pKi 94,121
⤷ pKi 8.1 (Ki 8.04x10-9 M) [94,121]
MSX-2 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.3 pKi 121
⤷ pKi 7.8 – 8.3 (Ki 1.45x10-8 – 5.38x10-9 M) [121]
PBF-509 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 7.6 – 7.9 pKi 49,87
⤷ pKi 7.9 (Ki 1.2x10-8 M) [49,87]
Description: Determined in a competitive radioligand binding assay using membranes prepared from HeLa cells expressing human A2A receptor.
pKi 7.6 (Ki 2.5x10-8 M) [49,87]
Description: Antagonism of rolipram-induced cAMP accummulation in CHO cells expressing the human A2A receptor, as measured using a proprietary enzymeimmunoassay.
LJ-4517 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.7 pKi 129
⤷ pKi 7.7 (Ki 1.83x10-8 M) [129]
Description: Displacing [3H]ZM-241385
KF 17837S Small molecule or natural product Hs Antagonist 7.7 pKi 32
⤷ pKi 7.7 [32]
istradefylline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 – 7.9 pKi 16,41
⤷ pKi 7.0 – 7.9 (Ki 9.12x10-8 – 1.2x10-8 M) [16,41]
CSC Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.3 pKi 54
⤷ pKi 7.3 (Ki 5.4x10-8 M) [54]
compound 10 [PMID: 31306001] Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 9
⤷ pKi 7.2 (Ki 6.8x10-8 M) [9]
Description: Binding affinity calculated by measuring displacement of specific [3H]ZM24138 binding at hA2AARs expressed in CHO cells.
mefloquine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Antagonist 7.0 pKi 145
⤷ pKi 7.0 (Ki 1.04x10-7 M) [145]
Description: Binding affinity determined by displacement of [3H]-CGS21680 from human A2A receptors by increasing concentrations of racemic mefloquine.
DPCPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 – 7.2 pKi 32,67-68,104,146
⤷ pKi 6.6 – 7.2 [32,67-68,104,146]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 55,135-136
⤷ pKi 6.8 [55,135-136]
LUF5981 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 16
⤷ pKi 6.7 (Ki 1.94x10-7 M) [16]
rolofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 – 7.0 pKi 61,109
⤷ pKi 6.2 – 7.0 (Ki 6.37x10-7 – 1.08x10-7 M) [61,109]
DPCPX Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 – 6.8 pKi 64,94
⤷ pKi 6.3 – 6.8 (Ki 5x10-7 – 1.57x10-7 M) [64,94]
derenofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 59
⤷ pKi 6.4 (Ki 3.98x10-7 M) [59]
rolofylline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 – 6.4 pKi 62,110
⤷ pKi 6.3 – 6.4 (Ki 5.1x10-7 – 3.8x10-7 M) [62,110]
KF26777 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 116
⤷ pKi 6.3 (Ki 4.7x10-7 M) [116]
MRS1754 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 65
⤷ pKi 6.3 (Ki 5.03x10-7 M) [65]
PSB36 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 pKi 146
⤷ pKi 6.3 (Ki 5.52x10-7 M) [146]
MRS1754 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.2 pKi 65
⤷ pKi 6.2 (Ki 6.12x10-7 M) [65]
CPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 63
⤷ pKi 6.2 [63]
ATL802 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 65
⤷ pKi 6.2 (Ki 6.54x10-7 M) [65]
CPFPX Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.1 pKi 51
⤷ pKi 6.1 (Ki 8.12x10-7 M) [51]
CPFPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 51
⤷ pKi 6.0 (Ki 9.4x10-7 M) [51]
PSB36 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 146
⤷ pKi 6.0 (Ki 9.8x10-7 M) [146]
MRE 2029F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 7
⤷ pKi <6.0 (Ki >1x10-6 M) [7]
galangin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.0 pKi 60
⤷ pKi 6.0 [60]
LAS38096 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 34,140
⤷ pKi <6.0 (Ki >1x10-6 M) [34,140]
LUF7602 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 150
⤷ pKi 5.9 (Ki 1.259x10-6 M) [150]
Description: Affinity determined from the displacement of specific [3H]ZM241385 binding on HEK293 cell membranes stably expressing human adenosine A2A receptors at 25 °C during 2 h of incubation.
FK-453 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 55
⤷ pKi 5.9 (Ki 1.3x10-6 M) [55]
PSB-11 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 105
⤷ pKi 5.9 (Ki 1.28x10-6 M) [105]
MRS1523 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.7 pKi 79
⤷ pKi 5.7 (Ki 2.05x10-6 M) [79]
PSB-11 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.7 pKi 105
⤷ pKi 5.7 (Ki 2.1x10-6 M) [105]
tonapofylline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.6 pKi 61
⤷ pKi 5.6 (Ki 2.44x10-6 M) [61]
PSB-10 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 105
⤷ pKi 5.6 (Ki 2.7x10-6 M) [105]
MRS1041 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 60
⤷ pKi 5.5 [60]
MRS1042 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 60
⤷ pKi 5.5 [60]
flavone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.5 pKi 60
⤷ pKi 5.5 [60]
theophylline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 5.2 – 5.8 pKi 32,53,67,135
⤷ pKi 5.2 – 5.8 [32,53,67,135]
CVT-6883 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 36
⤷ pKi 5.5 (Ki 3.28x10-6 M) [36]
MRS1523 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 pKi 79
⤷ pKi 5.4 (Ki 3.66x10-6 M) [79]
PSB-10 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.2 pKi 96
⤷ pKi 5.2 (Ki 6.04x10-6 M) [96]
MRS928 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 60
⤷ pKi 5.2 [60]
tonapofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 61
⤷ pKi 5.2 (Ki 6.41x10-6 M) [61]
caffeine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 4.6 – 5.6 pKi 1,