Page last updated: 2024-08-05 15:28:22

adenosine A1 receptor agonist

An agonist at the A1 receptor.

ChEBI ID: 65057

Members (3)

MemberDefinitionClass
adenosine monophosphateA purine ribonucleoside 5'-monophosphate having adenine as the nucleobase.adenosine 5'-monophosphate
adenosine-5'-(n-ethylcarboxamide)A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.N-ethyl-5'-carboxamidoadenosine
phenylisopropyladenosineA hydrocarbyladenosine in which adenosine is substituted at N-6 by a (2R)-1-phenylpropan-2-yl group. It is a potent adenosine A1 receptor agonist that exhibits neuroprotective and antinociceptive properties.(-)-N(6)-(2-phenylisopropyl)adenosine; (-)-n6-(2-phenylisopropyl)adenosine

Research

Studies (12,244)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19905,354 (43.73)18.7374
1990's1,995 (16.29)18.2507
2000's1,794 (14.65)29.6817
2010's1,497 (12.23)24.3611
2020's1,604 (13.10)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials261 (2.03%)5.53%
Reviews736 (5.74%)6.00%
Case Studies138 (1.08%)4.05%
Observational43 (0.34%)0.25%
Other11,650 (90.82%)84.16%

Protein Targets (113)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-synucleinHomo sapiens (human)Potency28.183811
AR proteinHomo sapiens (human)Potency12.235222
arylsulfatase AHomo sapiens (human)Potency4.318812
ATAD5 protein, partialHomo sapiens (human)Potency5.688445
Ataxin-2Homo sapiens (human)Potency8.912511
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency31.622811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.000011
chromobox protein homolog 1Homo sapiens (human)Potency2.989112
D(1A) dopamine receptorHomo sapiens (human)Potency1.158111
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency18.071933
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.353414
gemininHomo sapiens (human)Potency1.095422
glp-1 receptor, partialHomo sapiens (human)Potency2.771712
GLS proteinHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency10.682211
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.513111
IDH1Homo sapiens (human)Potency29.092911
importin subunit beta-1 isoform 1Homo sapiens (human)Potency6.513111
mitogen-activated protein kinase 1Homo sapiens (human)Potency8.912511
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency16.360111
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency125.892011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.298511
ras-related protein Rab-9AHomo sapiens (human)Potency16.360111
regulator of G-protein signaling 4Homo sapiens (human)Potency1.483313
relaxin receptor 1 isoform 1Homo sapiens (human)Potency6.408035
relaxin receptor 2 isoform 1Homo sapiens (human)Potency22.297412
snurportin-1Homo sapiens (human)Potency6.513111
TDP1 proteinHomo sapiens (human)Potency23.109311
thioredoxin reductaseRattus norvegicus (Norway rat)Potency2.107622
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency0.517411
USP1 protein, partialHomo sapiens (human)Potency15.848911
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.914522
vasopressin V1b receptorHomo sapiens (human)Potency11.903012

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
2-dehydropantoate 2-reductaseEscherichia coli K-12Ki6,300.000011
2-oxoglutarate receptor 1Rattus norvegicus (Norway rat)Ki0.032012
2'-deoxynucleoside 5'-phosphate N-hydrolase 1Homo sapiens (human)Ki19.200011
2'-deoxynucleoside 5'-phosphate N-hydrolase 1Rattus norvegicus (Norway rat)Ki40.000011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki10.000011
Adenosine receptor A1Gallus gallus (chicken)IC500.017011
Adenosine receptor A1Homo sapiens (human)IC500.277133
Adenosine receptor A1Rattus norvegicus (Norway rat)IC5014.06041014
Adenosine receptor A1Bos taurus (cattle)Ki0.011156
Adenosine receptor A1Homo sapiens (human)Ki0.15763641
Adenosine receptor A1Mus musculus (house mouse)Ki0.000411
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.09773346
Adenosine receptor A2aHomo sapiens (human)IC500.033688
Adenosine receptor A2aRattus norvegicus (Norway rat)IC500.1195614
Adenosine receptor A2aHomo sapiens (human)Ki0.25685262
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki1.05022231
Adenosine receptor A2bRattus norvegicus (Norway rat)IC500.1083412
Adenosine receptor A2bHomo sapiens (human)Ki0.86241013
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki1.51891423
Adenosine receptor A3Homo sapiens (human)IC504.38241515
Adenosine receptor A3Rattus norvegicus (Norway rat)IC500.049712
Adenosine receptor A3Homo sapiens (human)Ki0.43734652
Adenosine receptor A3Mus musculus (house mouse)Ki0.014111
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki0.09751212
Adenylate cyclase type 5Rattus norvegicus (Norway rat)Ki0.021814
Adenylate kinase 2, mitochondrialRattus norvegicus (Norway rat)Ki80.000011
Adenylate kinase isoenzyme 1 Rattus norvegicus (Norway rat)Ki580.000011
Aflatoxin B1 aldehyde reductase member 3Rattus norvegicus (Norway rat)Ki0.110011
Alcohol dehydrogenase E chainEquus caballus (horse)Ki38.000011
Alcohol dehydrogenase S chainEquus caballus (horse)Ki38.000011
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.012211
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.037011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.037011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.037011
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC500.440011
Chain A, ADENOSINE RECEPTOR A2AHomo sapiens (human)Ki0.013812
Chain A, ADP-dependent glucokinasePyrococcus furiosusKi60.000011
Chain A, phosphodiesterase-nucleotide pyrophosphataseXanthomonas citri pv. citri str. 306Ki260.000011
Chain A, Ribonuclease pancreaticBos taurus (cattle)Ki46.000012
Choline O-acetyltransferaseHomo sapiens (human)IC501,800,000,000.000011
Cytochrome P450 2C8Homo sapiens (human)Ki0.006811
Cytochrome P450 2C9 Homo sapiens (human)IC502.600011
Cytochrome P450 3A4Homo sapiens (human)Ki0.006811
EndoplasminHomo sapiens (human)Ki0.110011
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC502.64361111
Fructose-1,6-bisphosphatase 1Sus scrofa (pig)IC501.300022
Glycine--tRNA ligaseBombyx mori (domestic silkworm)Ki80.000011
Heat shock protein HSP 90-alphaHomo sapiens (human)Ki2.700011
high affinity choline transporter 1 isoform aHomo sapiens (human)IC501.861322
Histamine H3 receptorRattus norvegicus (Norway rat)IC500.800012
Inosine-5'-monophosphate dehydrogenaseEscherichia coli K-12Ki450.000011
L-lactate dehydrogenase A chainHomo sapiens (human)IC50500.000011
Protease Human immunodeficiency virus 1Ki0.000211
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC500.100011
ReninHomo sapiens (human)Ki0.000611
Thyroid hormone receptor betaRattus norvegicus (Norway rat)Ki0.063012
Transient receptor potential cation channel subfamily M member 2Homo sapiens (human)IC5070.000022
Transmembrane domain-containing protein TMIGD3Homo sapiens (human)Ki0.016011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
2-dehydropantoate 2-reductaseEscherichia coli K-12Kd5,000.000011
5'-AMP-activated protein kinase catalytic subunit alpha-1Homo sapiens (human)EC503.709522
5'-AMP-activated protein kinase catalytic subunit alpha-1Homo sapiens (human)Kd3.700011
5'-AMP-activated protein kinase catalytic subunit alpha-2Homo sapiens (human)EC503.650022
5'-AMP-activated protein kinase subunit beta-1Homo sapiens (human)EC502.939733
5'-AMP-activated protein kinase subunit beta-1Homo sapiens (human)Kd3.700011
5'-AMP-activated protein kinase subunit beta-2Homo sapiens (human)EC505.900011
5'-AMP-activated protein kinase subunit gamma-1Homo sapiens (human)EC502.939733
5'-AMP-activated protein kinase subunit gamma-1Homo sapiens (human)Kd3.700011
5'-AMP-activated protein kinase subunit gamma-2Homo sapiens (human)EC505.900011
5'-AMP-activated protein kinase subunit gamma-3Homo sapiens (human)EC505.900011
Adenosine receptor A1Cavia porcellus (domestic guinea pig)EC500.063111
Adenosine receptor A1Homo sapiens (human)EC500.15571919
Adenosine receptor A1Rattus norvegicus (Norway rat)EC5013.741244
Adenosine receptor A1Homo sapiens (human)Kd0.814377
Adenosine receptor A1Rattus norvegicus (Norway rat)Kd0.295111
Adenosine receptor A2aHomo sapiens (human)EC500.12891617
Adenosine receptor A2aRattus norvegicus (Norway rat)EC500.180733
Adenosine receptor A2bHomo sapiens (human)EC501.46242528
Adenosine receptor A2bRattus norvegicus (Norway rat)EC500.130011
Adenosine receptor A3Homo sapiens (human)EC5016.57041819
Adenosine receptor A3Mus musculus (house mouse)EC500.188011
Chain A, EndoplasminCanis lupus familiaris (dog)Kd0.200011
Chain A, GLYCOGEN PHOSPHORYLASE BOryctolagus cuniculus (rabbit)Kd101.800015
Chain B, GLYCOGEN PHOSPHORYLASE BOryctolagus cuniculus (rabbit)Kd85.333313
EndoplasminCanis lupus familiaris (dog)Kd2.800011
EndoplasminHomo sapiens (human)Kd0.530011
EndoplasminSus scrofa (pig)Kd0.200022
Heat shock protein HSP 90-alphaHomo sapiens (human)Kd30.000022
L-lactate dehydrogenase A chainHomo sapiens (human)Kd650.000011
Mitogen-activated protein kinase kinase kinase 7Homo sapiens (human)Kd245.000022
P2Y purinoceptor 1Homo sapiens (human)EC504.350012
P2Y purinoceptor 1Meleagris gallopavo (turkey)EC503.150012
P2Y purinoceptor 11Homo sapiens (human)EC5017.250011
P2Y purinoceptor 2Homo sapiens (human)EC501.892512
Protease Human immunodeficiency virus 1Kd0.001111

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5'-nucleotidaseHomo sapiens (human)Km14.000011
Adenosine deaminase-like proteinHomo sapiens (human)Km32.800011
Adenosine receptor A1Homo sapiens (human)Affinity constant0.051512
Adenosine receptor A1Rattus norvegicus (Norway rat)EC250.010011
Adenosine receptor A1Homo sapiens (human)KD hydro250.000011
Adenosine receptor A2aHomo sapiens (human)Affinity constant16.000012
Adenosine receptor A2aRattus norvegicus (Norway rat)EC250.010011
Adenosine receptor A2aRattus norvegicus (Norway rat)Ratio0.067214
Adenosine receptor A2bHomo sapiens (human)Affinity constant16.000012
Adenosine receptor A2bRattus norvegicus (Norway rat)EC250.010011
Adenosine receptor A2bRattus norvegicus (Norway rat)Ratio0.067114
Adenylate kinase 2, mitochondrialHomo sapiens (human)Km380.000011
Adenylate kinase 2, mitochondrialRattus norvegicus (Norway rat)Km85.000022
Adenylate kinase isoenzyme 1Homo sapiens (human)Km175.000011
Adenylate kinase isoenzyme 1 Rattus norvegicus (Norway rat)Km580.000011
Alkaline phosphatase, tissue-nonspecific isozymeHomo sapiens (human)Km441.000011
GTP:AMP phosphotransferase AK3, mitochondrialRattus norvegicus (Norway rat)Km85.000022