Page last updated: 2024-08-05 15:26:33

P2Y12 receptor antagonist

An antagonist at the P2Y12 receptor

ChEBI ID: 68563

Members (5)

MemberDefinitionClass
cangrelorA nucleoside triphosphate analogue that is 5'-O-[({[dichloro(phosphono)methyl](hydroxy)phosphoryl}oxy)(hydroxy)phosphoryl]adenosine carrying additional 2-(methylsulfanyl)ethyl and (3,3,3-trifluoropropyl)sulfanyl substituents at positions N6 and C2 respectively. Used (in the form of its tetrasodium salt) as an intravenous antiplatelet drug that prevents formation of harmful blood clots in the coronary arteries.cangrelor
clopidogrelA thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.clopidogrel
plavixclopidogrel sulfate
ticagrelorA triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.ticagrelor
ticlopidineA thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.ticlopidine

Research

Studies (13,100)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990309 (2.36)18.7374
1990's773 (5.90)18.2507
2000's3,424 (26.14)29.6817
2010's6,700 (51.15)24.3611
2020's1,894 (14.46)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,459 (19.09%)5.53%
Reviews4,053 (17.35%)6.00%
Case Studies2,086 (8.93%)4.05%
Observational625 (2.68%)0.25%
Other12,137 (51.96%)84.16%

Protein Targets (82)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency5.128822
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency3.981111
AR proteinHomo sapiens (human)Potency15.446733
ATAD5 protein, partialHomo sapiens (human)Potency29.081011
Chain A, Ferritin light chainEquus caballus (horse)Potency11.220212
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.118711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency5.972811
chromobox protein homolog 1Homo sapiens (human)Potency72.679612
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.039811
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.897511
cytochrome P450 2D6Homo sapiens (human)Potency0.549511
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.398111
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.848922
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency24.545411
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency10.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency19.952611
DNA polymerase kappa isoform 1Homo sapiens (human)Potency8.436811
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.022433
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency17.782811
EWS/FLI fusion proteinHomo sapiens (human)Potency23.492623
GVesicular stomatitis virusPotency4.897511
GABA theta subunitRattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.848911
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.848911
gemininHomo sapiens (human)Potency25.118911
glp-1 receptor, partialHomo sapiens (human)Potency7.943311
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.391411
heat shock protein beta-1Homo sapiens (human)Potency21.130011
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.897511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.897512
Interferon betaHomo sapiens (human)Potency4.897511
lamin isoform A-delta10Homo sapiens (human)Potency10.000011
LuciferasePhotinus pyralis (common eastern firefly)Potency8.709011
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency19.952611
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.832511
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.138233
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency89.125111
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency14.125411
pregnane X nuclear receptorHomo sapiens (human)Potency33.491511
progesterone receptorHomo sapiens (human)Potency18.833611
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency79.432811
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.849311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency13.516012
TDP1 proteinHomo sapiens (human)Potency29.474212
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency29.849322
thyroid stimulating hormone receptorHomo sapiens (human)Potency19.270433
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.000011
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency25.373522

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.382011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.143011
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.304011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.139011
Alpha-2C adrenergic receptorHomo sapiens (human)IC501.175011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.171011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Bile salt export pumpHomo sapiens (human)IC50293.237534
Bile salt export pumpRattus norvegicus (Norway rat)IC5049.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
CruzipainTrypanosoma cruziIC50211.500022
Cytochrome P450 2B6Homo sapiens (human)IC500.405022
Cytochrome P450 2B6Homo sapiens (human)Ki0.900023
Cytochrome P450 2C19Homo sapiens (human)IC500.667811
Cytochrome P450 2C19Homo sapiens (human)Ki34.866723
Cytochrome P450 2C8Homo sapiens (human)Ki26.350034
Cytochrome P450 2C9 Homo sapiens (human)IC5021.800011
Cytochrome P450 2D6Homo sapiens (human)IC506.292811
Cytochrome P450 2J2Homo sapiens (human)IC5021.800011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Ornithine decarboxylaseRattus norvegicus (Norway rat)IC500.000411
P2Y purinoceptor 12Homo sapiens (human)IC500.7214911
P2Y purinoceptor 12Homo sapiens (human)Ki0.008022
P2Y purinoceptor 13Homo sapiens (human)IC501.398011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.426011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.179011
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.562011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.299011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Liver carboxylesterase 1Homo sapiens (human)Km55.700011