Page last updated: 2024-08-05 15:10:53

anticoagulant

An agent that prevents blood clotting.

ChEBI ID: 50249

Members (38)

MemberDefinitionClass
3-methylquercetinA monomethoxyflavone that is quercetin in which the hydroxy group at position 3' is replaced by a methoxy group.isorhamnetin
acenocoumarolA hydroxycoumarin that is warfarin in which the hydrogen at position 4 of the phenyl substituent is replaced by a nitro group.acenocoumarol
acetylphenylalanyl-prolyl-boroarginineA C-terminal boronic acid petide that is N-acetyl-D-phenylalanyl-L-prolyl-L-arginine in which the C-termnal carboxy group has been replaced by a borono (-B(OH)2) group. A thrombin (Factor IIa) inhibitor, thereby acting as an anticoagulant.Ac-(D)Phe-Pro-boroArg-OH
alprostadilprostaglandin E1
anisindioneA cyclic beta-diketone consisting of indane-1,3-dione having a 4-methoxyphenyl substituent at the 4-position.anisindione
apixabanA pyrazolopyridine that is 7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide substituted at position 1 by a 4-methoxyphenyl group and at position 6 by a 4-(2-oxopiperidin-1-yl)phenyl group. It is used for the prevention and treatment of thromboembolic diseases.apixaban
aspirinA member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.acetylsalicylic acid
astaxanthineA carotenone that consists of beta,beta-carotene-4,4'-dione bearing two hydroxy substituents at positions 3 and 3' (the 3S,3'S diastereomer). A carotenoid pigment found mainly in animals (crustaceans, echinoderms) but also occurring in plants. It can occur free (as a red pigment), as an ester, or as a blue, brown or green chromoprotein.astaxanthin
atromentinA member of the class of dihydroxy-1,4-benzoquinones that is 2,5-dihydroxycyclohexa-2,5-diene-1,4-dione which is substituted by a 4-hydroxyphenyl group at positions 3 and 6. It is a mushroom pigment isolated from several fungi species and acts as a smooth muscle stimulant, and exhibits anticoagulant, antibacterial and antineoplastic properties.atromentin
betrixabanA secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade.betrixaban
bivalirudinA synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.bivalirudin
bl 4162aA 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions.anagrelide
cilostazolA lactam that is 3,4-dihydroquinolin-2(1H)-one in which the hydrogen at position 6 is substituted by a 4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy group.cilostazol
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
d-alpha tocopherolAn alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.(R,R,R)-alpha-tocopherol
dabigatranAn aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism.dabigatran
dabigatran etexilateAn aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.dabigatran etexilate
dabigatran etexilateAn aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.dabigatran etexilate
dicumarolA hydroxycoumarin that is methane in which two hydrogens have each been substituted by a 4-hydroxycoumarin-3-yl group. Related to warfarin, it has been used as an anticoagulant.dicoumarol
dieckolA phlorotannin isolated from a brown alga Ecklonia cava which exhibits antioxidant, hepatoprotective and anticoagulant activities.dieckol
edetic acidethylenediaminetetraacetic acid
edoxabanA monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism.edoxaban
eptifibatideA synthetic homodetic cyclic peptide comprising N(alpha)-(3-sulfanylpropanoyl)homoarginyl, glycyl, aspartyl, tryptophyl, prolyl and cysteinamide residues connected in sequence and cyclised via a disulfide bond. Derived from a protein found in the venom of the southeastern pygmy rattlesnake, Sistrurus miliarus barbouri, eptifibatide is an anti-coagulant that inhibits platelet aggregation by selectively blocking the platelet glycoprotein IIb/IIIa receptor, so preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. It is used in the management of unstable angina and in patients undergoing coronary angioplasty and stenting procedures.eptifibatide
fondaparinuxA synthetic pentasaccharide which, apart from the O-methyl group at the reducing end of the molecule, consists of monomeric sugar units which are identical to a sequence of five monomeric sugar units that can be isolated after either chemical or enzymatic cleavage of the polymeric glycosaminoglycans heparin and heparan sulfate.fondaparinux
ginsenoside rg2A ginsenoside found in Panax species that is dammarane which is substituted by hydroxy groups at the 3beta, 6alpha, 12beta and 20 pro-S positions, in which the hydroxy group at position 6 has been converted to the corresponding alpha-L-rhamnopyranosyl-(1->2)-beta-D-glucopyranoside, and in which a double bond has been introduced at the 24-25 position.ginsenoside Rg2
melagatranA member of the class of azetidines that is (2S)-azetidine 2-carboxylic acid in which the carboxylic acid has been converted to the amide corresponding to formal condensation with 4-(aminomethyl)benzenecarboximidamide and in which the hydrogen attached to the azetidine nitrogen is replaced by a (2R)-2-cyclohexyl-2-[(carboxymethyl)amino]acetyl group.melagatran
pd 0348292A member of the class of pyrrolidines that is (2R,4R)-N(1)-(p-chlorophenyl)-4-methoxypyrrolidine-1,2-dicarboxamide in which the nitrogen of the 2-carbamoyl group has been substituted by a 2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl group. It is a synthetic organic anticoagulant compound that targets activated factor Xa in the coagulation cascade.eribaxaban
phenindionephenindione
phenprocoumonA hydroxycoumarin that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenylpropyl group.phenprocoumon
plavixclopidogrel sulfate
plumbaginA hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively.plumbagin
rivaroxabanA monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.rivaroxaban
sodium citrate, anhydrousThe trisodium salt of citric acid.sodium citrate
suberosinA member of the class of coumarins in which the coumarin ring is substituted at positions 6 and 7 by a 3-methylbut-2-en-1-yl group and a methoxy group, respectively. A natural product found in Citropsis articulata.suberosin
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
tirofibanA member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.tirofiban
troglitazonetroglitazone
ximelagatranA member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.ximelagatran (hydroxylamine form); ximelagatran

Research

Studies (138,214)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199041,049 (29.70)18.7374
1990's21,415 (15.49)18.2507
2000's29,912 (21.64)29.6817
2010's34,714 (25.12)24.3611
2020's11,124 (8.05)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials18,366 (10.99%)5.53%
Reviews19,508 (11.68%)6.00%
Case Studies9,867 (5.91%)4.05%
Observational1,787 (1.07%)0.25%
Other117,530 (70.35%)84.16%

Protein Targets (347)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency24.172414
15-lipoxygenase, partialHomo sapiens (human)Potency3.162311
acetylcholinesteraseHomo sapiens (human)Potency31.012535
activating transcription factor 6Homo sapiens (human)Potency43.043112
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency20.492818
AR proteinHomo sapiens (human)Potency19.49891144
ATAD5 protein, partialHomo sapiens (human)Potency26.256723
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency7.568611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency6.365725
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency86.288513
caspase-1 isoform alpha precursorHomo sapiens (human)Potency22.106012
Caspase-7Homo sapiens (human)Potency19.952611
Cellular tumor antigen p53Homo sapiens (human)Potency23.1089312
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency8.473729
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency20.804214
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency46.669225
Chain A, Ferritin light chainEquus caballus (horse)Potency14.942513
Chain A, HADH2 proteinHomo sapiens (human)Potency30.736913
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.118711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency24.806818
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency0.111911
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency27.470916
Chain B, HADH2 proteinHomo sapiens (human)Potency30.736913
chromobox protein homolog 1Homo sapiens (human)Potency63.342513
cytochrome P450 2C19 precursorHomo sapiens (human)Potency5.019912
cytochrome P450 2C9 precursorHomo sapiens (human)Potency19.917912
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.936318
cytochrome P450 2D6Homo sapiens (human)Potency20.024416
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.398111
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency17.3831213
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.019019
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency35.093313
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency10.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency54.538812
DNA polymerase kappa isoform 1Homo sapiens (human)Potency23.260014
dual specificity mitogen-activated protein kinase kinase 1Homo sapiens (human)Potency12.589311
endonuclease IVEscherichia coliPotency12.589311
Endothelin receptor type BRattus norvegicus (Norway rat)Potency17.782811
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency17.782811
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.53331142
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency15.669637
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency22.8389840
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.6405110
EWS/FLI fusion proteinHomo sapiens (human)Potency15.3602419
farnesoid X nuclear receptorHomo sapiens (human)Potency39.132934
flap endonuclease 1Homo sapiens (human)Potency56.234111
Fumarate hydrataseHomo sapiens (human)Potency33.173411
GVesicular stomatitis virusPotency4.936318
GABA theta subunitRattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency17.040717
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency17.040717
gemininHomo sapiens (human)Potency13.012526
GLI family zinc finger 3Homo sapiens (human)Potency19.129427
glp-1 receptor, partialHomo sapiens (human)Potency7.943311
GLS proteinHomo sapiens (human)Potency18.623112
glucocerebrosidaseHomo sapiens (human)Potency0.354811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency20.643138
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency22.685416
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency1.458111
Guanine nucleotide-binding protein GHomo sapiens (human)Potency13.699612
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency5.227612
heat shock protein beta-1Homo sapiens (human)Potency31.089525
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency14.6604210
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency34.090814
histone deacetylase 9 isoform 3Homo sapiens (human)Potency20.236123
Histone H2A.xCricetulus griseus (Chinese hamster)Potency42.880014
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.936318
hypothetical protein, conservedTrypanosoma bruceiPotency50.118711
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency6.310612
IDH1Homo sapiens (human)Potency0.461111
importin subunit beta-1 isoform 1Homo sapiens (human)Potency1.458111
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.9363116
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.778113
Integrin alpha-IIbHomo sapiens (human)Potency8.058115
Integrin beta-3Homo sapiens (human)Potency8.058115
Interferon betaHomo sapiens (human)Potency5.2056313
interleukin 8Homo sapiens (human)Potency74.978011
lamin isoform A-delta10Homo sapiens (human)Potency5.911915
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency23.392339
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency11.220211
M-phase phosphoprotein 8Homo sapiens (human)Potency1.000011
Microtubule-associated protein tauHomo sapiens (human)Potency13.5511210
mitogen-activated protein kinase 1Homo sapiens (human)Potency8.637836
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency2.238711
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency9.391412
neuropeptide S receptor isoform AHomo sapiens (human)Potency19.952611
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency17.900812
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency5.623411
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency17.4813311
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency20.596211
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency32.026914
Nuclear receptor ROR-gammaHomo sapiens (human)Potency8.412711
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency9.753529
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency22.4302314
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency66.896812
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency21.189212
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency6.0515411
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency19.088437
phosphopantetheinyl transferaseBacillus subtilisPotency35.481311
polyproteinZika virusPotency33.173411
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency6.774012
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency11.776813
PPM1D proteinHomo sapiens (human)Potency0.082912
pregnane X nuclear receptorHomo sapiens (human)Potency26.142737
progesterone receptorHomo sapiens (human)Potency15.069325
pyruvate kinaseLeishmania mexicana mexicanaPotency17.782822
RAF proto-oncogene serine/threonine-protein kinase isoform bHomo sapiens (human)Potency25.118911
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency5.011911
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency79.432811
RAR-related orphan receptor gammaMus musculus (house mouse)Potency14.0020215
ras-related protein Rab-9AHomo sapiens (human)Potency4.466811
regulator of G-protein signaling 4Homo sapiens (human)Potency23.778111
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency27.9444212
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.1872310
SMAD family member 2Homo sapiens (human)Potency15.564625
SMAD family member 3Homo sapiens (human)Potency15.564625
snurportin-1Homo sapiens (human)Potency1.458111
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency23.412016
survival motor neuron protein isoform dHomo sapiens (human)Potency11.795414
TDP1 proteinHomo sapiens (human)Potency16.8732219
thioredoxin glutathione reductaseSchistosoma mansoniPotency79.432811
thioredoxin reductaseRattus norvegicus (Norway rat)Potency12.561024
ThrombopoietinHomo sapiens (human)Potency15.848922
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency21.539739
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency19.952611
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.6751515
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Potency12.589311
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)Potency12.589311
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Potency12.589311
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.000011
USP1 protein, partialHomo sapiens (human)Potency31.947915
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency25.155526
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency17.562624
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency12.339513
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency22.685416

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC502.045022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC506.300011
3-oxoacyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC508.300011
4-aminobutyrate aminotransferase, mitochondrialRattus norvegicus (Norway rat)IC502.400012
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC501.312011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.835011
60 kDa chaperoninEscherichia coli K-12IC50250.000011
60 kDa chaperonin Escherichia coliIC502.045022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC506.300011
Adenosine receptor A1Rattus norvegicus (Norway rat)IC505,000.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)IC505,000.000011
Adenosine receptor A3Homo sapiens (human)IC505.208011
Adenosine receptor A3Homo sapiens (human)Ki2.943011
Aldo-keto reductase family 1 member B1Sus scrofa (pig)IC5095.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC505.208011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki2.943011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC505.208011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.943011
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
Amine oxidase [flavin-containing] AHomo sapiens (human)IC503.000012
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki10.500011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Ki4.800011
Amine oxidase [flavin-containing] BHomo sapiens (human)IC502.070022
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki9.500011
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki10.900011
Amyloid-beta precursor proteinHomo sapiens (human)IC5018.050022
Angiotensin-converting enzyme Homo sapiens (human)IC5014.000011
ATP phosphoribosyltransferaseMycobacterium tuberculosis H37RvKi60.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50103.271417
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC501.285011
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC501.285011
Aurora kinase BHomo sapiens (human)IC504.340011
Beta-lactamase Bacillus anthracisIC501,060.000011
Beta-lactamase Pseudomonas aeruginosaIC5027.900011
Beta-lactamase VIM-1 Pseudomonas aeruginosaIC509.300011
Beta-secretase 1Homo sapiens (human)IC50251.105022
Beta-secretase 1Homo sapiens (human)Ki1.500011
Bile salt export pumpHomo sapiens (human)IC5065.2694717
Bile salt export pumpRattus norvegicus (Norway rat)IC5021.166723
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC501,000.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC501,000.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC501,000.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000016
Carbonic anhydraseCandida albicans SC5314Ki39.100011
Carbonic anhydrase 1Homo sapiens (human)IC502,710.000011
Carbonic anhydrase 1Homo sapiens (human)Ki2,516.666733
Carbonic anhydrase 12Homo sapiens (human)Ki0.137422
Carbonic anhydrase 2Homo sapiens (human)IC50580.485022
Carbonic anhydrase 2Homo sapiens (human)Ki1,598.088055
Carbonic anhydrase 4Homo sapiens (human)Ki0.156022
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki1,670.000011
Carbonic anhydrase 7Homo sapiens (human)Ki0.004411
Carbonic anhydrase 9Homo sapiens (human)Ki4,930.000011
Cationic trypsinBos taurus (cattle)IC500.011211
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC5034.000022
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC500.27101010
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC500.300799
Chain A, Activated Factor Xa Heavy ChainHomo sapiens (human)Ki0.000411
Chain A, Coagulation factor X (EC 3.4.21.6) (Stuart factor) (Stuart-Prower factor)Homo sapiens (human)Ki0.000111
Chain H, ProthrombinHomo sapiens (human)Ki0.004012
CholinesteraseHomo sapiens (human)IC500.002611
Coagulation factor VIIHomo sapiens (human)IC503.300011
Coagulation factor XHomo sapiens (human)IC502.55022022
Coagulation factor XHomo sapiens (human)Ki0.52931829
Coagulation factor XOryctolagus cuniculus (rabbit)Ki0.000211
Coagulation factor XIHomo sapiens (human)IC5020.000011
Coagulation factor XIIHomo sapiens (human)IC5033.000012
CruzipainTrypanosoma cruziIC50211.500022
Cytochrome P450 1A1Homo sapiens (human)IC501.413022
Cytochrome P450 1A1Homo sapiens (human)Ki2.560011
Cytochrome P450 1A2Homo sapiens (human)IC501.860522
Cytochrome P450 1A2Homo sapiens (human)Ki2.360011
Cytochrome P450 1B1Homo sapiens (human)IC503.083522
Cytochrome P450 2B6Homo sapiens (human)IC500.405022
Cytochrome P450 2B6Homo sapiens (human)Ki0.900023
Cytochrome P450 2C19Homo sapiens (human)IC505.333922
Cytochrome P450 2C19Homo sapiens (human)Ki34.866723
Cytochrome P450 2C8Homo sapiens (human)Ki26.350034
Cytochrome P450 2C9 Homo sapiens (human)IC509.220035
Cytochrome P450 2C9 Homo sapiens (human)Ki1.250022
Cytochrome P450 2D6Homo sapiens (human)IC50181.430933
Cytochrome P450 2J2Homo sapiens (human)IC5021.800011
Cytochrome P450 3A4Homo sapiens (human)IC5010.000011
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC5017.300012
Enoyl-[acyl-carrier-protein] reductase [NADH] Francisella tularensis subsp. tularensis SCHU S4IC5047.000011
Enoyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC505.000011
Epidermal growth factor receptorHomo sapiens (human)IC5010.000011
Eyes absent homolog 2Homo sapiens (human)IC50386.250044
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki2,064.000022
Forkhead box protein M1Homo sapiens (human)IC50122.400011
Forkhead box protein M1Homo sapiens (human)Ki0.052011
G-protein coupled receptor 35Homo sapiens (human)Ki0.039011
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)Ki1.000011
Gag-Pol polyproteinHuman immunodeficiency virus type 2 (ISOLATE ROD)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.350011
Glutathione hydrolase 1 proenzymeHomo sapiens (human)IC5036.000011
Glutathione S-transferase PHomo sapiens (human)IC500.500011
Histone acetyltransferase KAT2BHomo sapiens (human)IC5050.000033
Histone acetyltransferase p300Homo sapiens (human)IC5015.500044
Indoleamine 2,3-dioxygenase 1Mus musculus (house mouse)IC5061.000011
Indoleamine 2,3-dioxygenase 2Mus musculus (house mouse)IC504.500011
Inositol hexakisphosphate kinase 2Homo sapiens (human)IC500.500011
Inositol polyphosphate multikinaseHomo sapiens (human)IC502.200011
Integrase Human immunodeficiency virus 1IC50166.666723
Integrin alpha-5Homo sapiens (human)IC50300.000022
Integrin alpha-IIbHomo sapiens (human)IC503.31262833
Integrin alpha-V Homo sapiens (human)IC50113.835266
Integrin beta-1Homo sapiens (human)IC50300.000022
Integrin beta-3Homo sapiens (human)IC5020.31613439
Integrin beta-3 Rattus norvegicus (Norway rat)IC500.130011
Integrin subunit alpha 2bRattus norvegicus (Norway rat)IC500.130011
M-phase inducer phosphatase 1Homo sapiens (human)IC500.700011
M-phase inducer phosphatase 2Homo sapiens (human)IC503.100011
Metallo-beta-lactamase VIM-13Pseudomonas aeruginosaIC50252.600011
Mitogen-activated protein kinase 1Homo sapiens (human)IC502.832012
Mitogen-activated protein kinase 10Homo sapiens (human)IC5013.200012
Mitogen-activated protein kinase 14Homo sapiens (human)IC5013.200012
Mitogen-activated protein kinase kinase kinase 14Homo sapiens (human)IC50100.000011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC508.100011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5025.300011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5087.414317
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC5010.000011
MyeloperoxidaseHomo sapiens (human)IC50200.000011
NADHomo sapiens (human)IC500.258578
NADRattus norvegicus (Norway rat)Ki0.001011
Nicotinate phosphoribosyltransferaseHomo sapiens (human)Ki0.000511
Oligo-1,6-glucosidase IMA1Saccharomyces cerevisiae S288CIC50160.000011
P2Y purinoceptor 12Homo sapiens (human)IC502.400011
Pancreatic triacylglycerol lipaseSus scrofa (pig)IC5070.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC501.030066
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.316855
PlasminogenHomo sapiens (human)IC505.373323
PlasminogenHomo sapiens (human)Ki1.398333
Polyphenol oxidase 2Agaricus bisporusIC5020.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC508.900022
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki1.800011
Proprotein convertase subtilisin/kexin type 7Homo sapiens (human)IC501.300011
Prostacyclin receptorHomo sapiens (human)Ki2.612534
Prostaglandin E2 receptor EP1 subtypeMus musculus (house mouse)Ki0.037534
Prostaglandin E2 receptor EP2 subtypeMus musculus (house mouse)Ki0.047834
Prostaglandin E2 receptor EP3 subtypeMus musculus (house mouse)Ki0.005033
Prostaglandin E2 receptor EP4 subtypeMus musculus (house mouse)Ki0.003234
Prostaglandin G/H synthase 1Homo sapiens (human)IC50337.14521010
Prostaglandin G/H synthase 1Ovis aries (sheep)IC501,813.84453740
Prostaglandin G/H synthase 1Homo sapiens (human)Ki62.000011
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC502,018.725056
Prostaglandin G/H synthase 2Homo sapiens (human)IC50907.52352426
Prostaglandin G/H synthase 2Ovis aries (sheep)IC50523.74682222
Prostaglandin G/H synthase 2Homo sapiens (human)Ki52.000011
Prostaglandin G/H synthase 2 Bos taurus (cattle)IC501,500.000012
Prostaglandin-H2 D-isomeraseMus musculus (house mouse)IC501,500.000011
Protease Human immunodeficiency virus 1IC501.000011
Protease Human immunodeficiency virus 1Ki0.700244
ProthrombinHomo sapiens (human)IC501.97352426
ProthrombinHomo sapiens (human)Ki0.51721820
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC5030.800011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5017.100011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5029.300033
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi2.400011
Rho-associated protein kinase 2Rattus norvegicus (Norway rat)IC50100.000012
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC5010.500022
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)Ki60.000011
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC501.375012
Sentrin-specific protease 1Homo sapiens (human)IC504.945022
Serine protease hepsinHomo sapiens (human)Ki0.835011
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
Solute carrier family 22 member 2Homo sapiens (human)IC504.700011
Solute carrier family 22 member 20Mus musculus (house mouse)Ki101.664512
Solute carrier family 22 member 6Mus musculus (house mouse)Ki689.415512
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki428.000011
Solute carrier organic anion transporter family member 2B1Rattus norvegicus (Norway rat)IC500.035811
Substance-P receptorCavia porcellus (domestic guinea pig)IC502.400011
Suppressor of tumorigenicity 14 proteinHomo sapiens (human)Ki3.350011
Thiosulfate sulfurtransferaseHomo sapiens (human)IC500.060011
Thromboxane-A synthase Homo sapiens (human)IC502.966011
Thromboxane-A synthase Homo sapiens (human)Ki0.100011
Tissue-type plasminogen activatorHomo sapiens (human)IC5010.000011
Tissue-type plasminogen activatorHomo sapiens (human)Ki15.923333
Trypanothione reductaseTrypanosoma cruziIC5028.000022
Trypsin-1Homo sapiens (human)IC500.011912
Trypsin-1Homo sapiens (human)Ki0.718966
Trypsin-2Homo sapiens (human)IC500.011912
Trypsin-2Homo sapiens (human)Ki1.076244
Trypsin-3Homo sapiens (human)IC500.011912
Trypsin-3Homo sapiens (human)Ki1.076244
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5055.000011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)Ki20.000011
UreaseCanavalia ensiformis (jack bean)IC5015.072822
Urokinase-type plasminogen activatorHomo sapiens (human)Ki6.300011
Urotensin-2 receptorRattus norvegicus (Norway rat)IC500.300012
Vitamin K-dependent protein CHomo sapiens (human)IC505.650022
Vitamin K-dependent protein CHomo sapiens (human)Ki20.930011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5091.200011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC5091.200011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC5091.200011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC5091.200011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC502.510011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-tocopherol transfer proteinHomo sapiens (human)Kd2.420011
cell division cycle 42 (GTP binding protein, 25kDa), partialHomo sapiens (human)EC5030.000022
Chain A, Coagulation factor X, heavy chainHomo sapiens (human)Kd0.000311
Chain A, Phospholipase A2 isoform 3Naja sagittiferaKd6.400011
Dual specificity mitogen-activated protein kinase kinase 7Homo sapiens (human)Kd14.000011
G-protein coupled receptor 35Homo sapiens (human)EC504.126733
GTP-binding protein (rab7)Canis lupus familiaris (dog)EC5030.000011
Integrin alpha-IIbHomo sapiens (human)Kd0.010033
Integrin alpha-V Homo sapiens (human)Kd0.120011
Integrin beta-3Homo sapiens (human)Kd0.037544
Mitogen-activated protein kinase 14Homo sapiens (human)EC501.000011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)EC500.780012
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)EC500.780012
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)EC500.780012
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)EC500.780012
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)EC500.780012
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5015.800033
Nuclear receptor subfamily 4 group A member 2Homo sapiens (human)EC503.000022
Nuclear receptor subfamily 4 group A member 2Mus musculus (house mouse)EC503.000022
Nuclear receptor subfamily 4 group A member 2Rattus norvegicus (Norway rat)EC503.000022
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC501.10001919
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC500.890022
Prostacyclin receptorHomo sapiens (human)EC500.001811
Prostaglandin E2 receptor EP2 subtypeMus musculus (house mouse)EC500.002611
Prostaglandin E2 receptor EP4 subtypeMus musculus (house mouse)EC500.002923
ProthrombinHomo sapiens (human)Kd0.000722
Rac1 proteinHomo sapiens (human)EC5030.000022
ras protein, partialHomo sapiens (human)EC5030.000022
Ras-related protein Rab-2ACanis lupus familiaris (dog)EC5030.000011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKd10.300011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)EC5030.000012
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)EC5030.000022
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC500.460011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)Km74.000011
DNA topoisomerase 1Homo sapiens (human)MIC50.000011
Integrin alpha-IIbHomo sapiens (human)ED500.001011
Integrin beta-3Homo sapiens (human)ED500.001011
Liver carboxylesterase 1Homo sapiens (human)Km55.700011
Multidrug resistance-associated protein 4Homo sapiens (human)Km2.100011
NADHomo sapiens (human)Activity11.000011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Fold activation1.120011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Fold activation3.160011
Platelet-activating factor acetylhydrolaseHomo sapiens (human)Km74.000015
Solute carrier organic anion transporter family member 2A1Homo sapiens (human)K1/20.082011
Solute carrier organic anion transporter family member 2A1Rattus norvegicus (Norway rat)Km0.070011
Solute carrier organic anion transporter family member 3A1Homo sapiens (human)Km0.048511
Trypanothione reductaseTrypanosoma cruziKm15.000011
Trypanothione reductaseTrypanosoma cruzix fold525.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km58.000011
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Km11.000011