Page last updated: 2024-08-05 15:33:50

estrogen receptor antagonist

An antagonist at the estrogen receptor.

ChEBI ID: 50792

Members (9)

MemberDefinitionClass
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diolA carbotetracyclic compound that is 5,6,11,12-tetrahydrochrysene substituted by hydroxy groups at positions 2 and 8 and by ethyl groups at positions 5 and 11 (the 5R,11R-stereoisomer). It is an agonist of ER-alpha and antagonist of ER-beta receptors.(R,R)-5,11-diethyl-5,6,11,12-tetrahydro-2,8-chrysenediol
afimoxifeneA tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.afimoxifene
diallyl trisulfideAn organic trisulfide that is trisulfane in which both of the hydrogens are replaced by allyl groups. A component of the essential oil of garlic and a major component of the traditional Chinese medicine allitridium, it exhibits antifungal, antitumour and antioxidant activitydiallyl trisulfide
fulvestrantA 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.fulvestrant
ici 164384A 3-hydroxy steroid that is 17beta-estradiol substituted by a 11-[butyl(methyl)amino]-11-oxoundecyl group at position 7R. It is a steroidal antioestrogen that inhibits the cell proliferation of breast-carcinoma cell lines.ICI-164384
lasofoxifeneA member of the class of tetralins that is 5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogens at positions 5 and 6 are replaced by 4-[2-(pyrrolidin-1-yl)ethoxy]phenyl and phenyl groups, respectively (the 5R,6S-stereoisomer). It is a selective estrogen receptor modulator indicated for the prevention and treatment of osteoporosis in post-menopausal women.lasofoxifene
ly 117018A member of the class of 1-benzothiophenes that is raloxifene in which the piperidin-1-yl group has been replaced by a pyrrolidin-1-yl group.LY 117018
ru 58668A 17beta-hydroxy steroid that is 17beta-estradiol in the the hydrogen at the 11beta position has been replaced by a p-({5-[(4,4,5,5,5-pentafluoropentyl)sulfonyl]pentyl}oxy)phenyl group. RU 58668 is a pure anti-estrogen that downregulates estrogen receptor expression (IC50 = 0.04 nM).RU 58668
tamoxifentamoxifen

Research

Studies (22,134)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,520 (11.39)18.7374
1990's4,589 (20.73)18.2507
2000's6,851 (30.95)29.6817
2010's6,462 (29.19)24.3611
2020's1,712 (7.73)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,462 (9.69%)5.53%
Reviews3,049 (12.00%)6.00%
Case Studies1,303 (5.13%)4.05%
Observational74 (0.29%)0.25%
Other18,526 (72.90%)84.16%

Protein Targets (275)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency29.330113
15-lipoxygenase, partialHomo sapiens (human)Potency10.000011
67.9K proteinVaccinia virusPotency10.451013
acetylcholinesteraseHomo sapiens (human)Potency59.521637
acid sphingomyelinaseHomo sapiens (human)Potency25.118911
activating transcription factor 6Homo sapiens (human)Potency42.842727
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.985613
alpha-galactosidaseHomo sapiens (human)Potency32.815235
Alpha-synucleinHomo sapiens (human)Potency18.356412
Amyloid-beta precursor proteinHomo sapiens (human)Potency29.092911
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency35.481312
AR proteinHomo sapiens (human)Potency30.95481029
aryl hydrocarbon receptorHomo sapiens (human)Potency25.752311
arylsulfatase AHomo sapiens (human)Potency5.066912
ATAD5 protein, partialHomo sapiens (human)Potency23.955723
Ataxin-2Homo sapiens (human)Potency47.596925
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency69.215624
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency10.691011
Bloom syndrome protein isoform 1Homo sapiens (human)Potency17.782822
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.986813
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency41.016313
caspase-3Cricetulus griseus (Chinese hamster)Potency36.555813
caspase-3Homo sapiens (human)Potency41.016313
Caspase-7Cricetulus griseus (Chinese hamster)Potency36.555813
Cellular tumor antigen p53Homo sapiens (human)Potency42.2158311
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency22.921024
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency26.651412
Chain A, Beta-lactamaseEscherichia coli K-12Potency14.986723
Chain A, CruzipainTrypanosoma cruziPotency28.183811
Chain A, Ferritin light chainEquus caballus (horse)Potency28.454224
Chain A, HADH2 proteinHomo sapiens (human)Potency25.118922
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.340413
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency100.000011
Chain B, HADH2 proteinHomo sapiens (human)Potency25.118922
chromobox protein homolog 1Homo sapiens (human)Potency35.638323
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.589311
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.162311
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.380311
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency35.716812
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency29.094126
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.500822
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency2.429315
D(1A) dopamine receptorHomo sapiens (human)Potency4.157034
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency25.118911
DNA polymerase eta isoform 1Homo sapiens (human)Potency100.000011
DNA polymerase III, partialBacillus subtilisPotency29.934911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency64.091912
dopamine D1 receptorHomo sapiens (human)Potency23.109311
estrogen nuclear receptor alphaHomo sapiens (human)Potency14.62271249
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency48.0423312
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.59981043
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.878319
farnesoid X nuclear receptorHomo sapiens (human)Potency44.3332510
Fumarate hydrataseHomo sapiens (human)Potency35.481311
GVesicular stomatitis virusPotency1.380311
GABA theta subunitRattus norvegicus (Norway rat)Potency29.094113
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency29.094113
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency29.094113
gemininHomo sapiens (human)Potency16.343047
GLI family zinc finger 3Homo sapiens (human)Potency11.9463312
glp-1 receptor, partialHomo sapiens (human)Potency18.063612
GLS proteinHomo sapiens (human)Potency11.070523
glucocerebrosidaseHomo sapiens (human)Potency25.657216
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency29.9233413
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency1.481016
heat shock protein beta-1Homo sapiens (human)Potency46.291725
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency5.2462211
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency22.387211
Histone H2A.xCricetulus griseus (Chinese hamster)Potency46.992025
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.380311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency49.090526
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency25.118922
IDH1Homo sapiens (human)Potency17.025513
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.380312
Integrin alpha-IIbHomo sapiens (human)Potency23.735812
Integrin beta-3Homo sapiens (human)Potency23.735812
Interferon betaHomo sapiens (human)Potency22.911324
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency23.842723
lethal factor (plasmid)Bacillus anthracis str. A2012Potency23.735812
M-phase phosphoprotein 8Homo sapiens (human)Potency28.336812
Microtubule-associated protein tauHomo sapiens (human)Potency21.811226
mitogen-activated protein kinase 1Homo sapiens (human)Potency23.753122
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.294722
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.000012
NFKB1 protein, partialHomo sapiens (human)Potency10.000022
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.610112
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047912
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency34.369938
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency36.426112
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency36.167626
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency21.977426
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency28.183811
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency48.8568310
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.118711
ParkinHomo sapiens (human)Potency25.929011
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency37.933011
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency57.1173510
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency40.283258
phosphopantetheinyl transferaseBacillus subtilisPotency47.283826
plasminogen precursorMus musculus (house mouse)Potency5.380812
polyproteinZika virusPotency35.481311
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency15.848911
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency6.027614
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency25.118911
PPM1D proteinHomo sapiens (human)Potency30.088312
pregnane X nuclear receptorHomo sapiens (human)Potency7.816138
pregnane X receptorRattus norvegicus (Norway rat)Potency55.527812
progesterone receptorHomo sapiens (human)Potency44.9726310
putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)Potency39.810711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency20.1698212
ras-related protein Rab-9AHomo sapiens (human)Potency75.023812
regulator of G-protein signaling 4Homo sapiens (human)Potency15.271413
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency53.027839
retinoid X nuclear receptor alphaHomo sapiens (human)Potency34.089348
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.094945
SMAD family member 2Homo sapiens (human)Potency61.133437
SMAD family member 3Homo sapiens (human)Potency61.133437
Smad3Homo sapiens (human)Potency35.481312
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TAR DNA-binding protein 43Homo sapiens (human)Potency35.481311
TDP1 proteinHomo sapiens (human)Potency21.053029
thioredoxin reductaseRattus norvegicus (Norway rat)Potency33.668149
ThrombopoietinHomo sapiens (human)Potency5.011922
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency7.3522311
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency16.414823
thyroid stimulating hormone receptorHomo sapiens (human)Potency47.2922610
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency29.462925
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency11.220211
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency25.118911
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency5.380812
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency5.380812
USP1 protein, partialHomo sapiens (human)Potency59.664912
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency22.227826
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency58.062145
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.239415
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency1.481016
VprHuman immunodeficiency virus 1Potency35.481311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)IC500.012011
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.005011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC5012.160011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki6.949011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC5012.160011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki6.949011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC504.801011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki1.372011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC502.084011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki1.326011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.460011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.241011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.460011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.241011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC502.679011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.142522
7-dehydrocholesterol reductaseHomo sapiens (human)IC500.012011
Adenosine receptor A1Homo sapiens (human)IC5023.767011
Adenosine receptor A1Homo sapiens (human)Ki13.864011
Adenosine receptor A2aHomo sapiens (human)IC507.099011
Adenosine receptor A2aHomo sapiens (human)Ki3.985011
Adenosine receptor A3Homo sapiens (human)IC503.701011
Adenosine receptor A3Homo sapiens (human)Ki2.092011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC501.472011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.459011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC503.701011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki2.092011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC503.701011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.092011
Alpha-1D adrenergic receptorHomo sapiens (human)IC504.982011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki2.449011
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.935011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.726011
Alpha-2B adrenergic receptorHomo sapiens (human)IC503.518011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.606011
Androgen receptorRattus norvegicus (Norway rat)IC5017.342322
Androgen receptorRattus norvegicus (Norway rat)Ki15.108011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC500.967011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki0.792211
AromataseHomo sapiens (human)IC50530.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
ATP-dependent translocase ABCB1Homo sapiens (human)IC5019.725044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki0.100011
B2 bradykinin receptorHomo sapiens (human)IC5020.356011
B2 bradykinin receptorHomo sapiens (human)Ki12.048011
Beta-1 adrenergic receptorHomo sapiens (human)IC5017.289011
Beta-1 adrenergic receptorHomo sapiens (human)Ki9.984011
Beta-3 adrenergic receptorHomo sapiens (human)IC507.703011
Beta-3 adrenergic receptorHomo sapiens (human)Ki5.778011
Beta-lactamase TEMEscherichia coliIC5055.900011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC500.006011
Bifunctional epoxide hydrolase 2Homo sapiens (human)Ki0.026011
Bile acid receptorHomo sapiens (human)IC501.050012
Bile salt export pumpHomo sapiens (human)IC5074.950056
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi1.500011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Chain A, CES1 proteinHomo sapiens (human)Ki15.200011
Cytochrome P450 2B6Homo sapiens (human)Ki0.900011
Cytochrome P450 3A4Homo sapiens (human)Ki0.200011
D(1A) dopamine receptorHomo sapiens (human)IC508.502011
D(1A) dopamine receptorHomo sapiens (human)Ki4.251011
D(2) dopamine receptorHomo sapiens (human)IC5013.885011
D(2) dopamine receptorHomo sapiens (human)Ki4.628011
D(3) dopamine receptorHomo sapiens (human)IC501.072011
D(3) dopamine receptorHomo sapiens (human)Ki0.364011
D(4) dopamine receptorHomo sapiens (human)IC5011.161011
D(4) dopamine receptorHomo sapiens (human)Ki3.913011
Delta-type opioid receptorHomo sapiens (human)IC5013.339011
Delta-type opioid receptorHomo sapiens (human)Ki4.702011
Emopamil-binding protein-likeHomo sapiens (human)Ki0.002811
Epidermal growth factor receptorHomo sapiens (human)IC503.553011
Estrogen receptorHomo sapiens (human)IC500.483182102
Estrogen receptorRattus norvegicus (Norway rat)IC500.009423
Estrogen receptorHomo sapiens (human)Ki0.0253810
Estrogen receptor betaHomo sapiens (human)IC500.59354148
Estrogen receptor betaRattus norvegicus (Norway rat)IC500.011212
Estrogen receptor betaHomo sapiens (human)Ki0.0222810
Estrogen-related receptor gammaHomo sapiens (human)IC500.021934
Fatty acid synthaseGallus gallus (chicken)IC508.370022
Histamine H2 receptorHomo sapiens (human)IC509.396011
Histamine H2 receptorHomo sapiens (human)Ki9.240011
Kappa-type opioid receptorHomo sapiens (human)IC5015.629011
Kappa-type opioid receptorHomo sapiens (human)Ki6.252011
Melanocortin receptor 3Homo sapiens (human)IC5019.856011
Melanocortin receptor 3Homo sapiens (human)Ki17.329011
Melanocortin receptor 4Homo sapiens (human)IC5030.481011
Melanocortin receptor 4Homo sapiens (human)Ki29.308011
Melanocortin receptor 5Homo sapiens (human)IC5026.529011
Melanocortin receptor 5Homo sapiens (human)Ki24.886011
Mu-type opioid receptorHomo sapiens (human)IC5017.594011
Mu-type opioid receptorHomo sapiens (human)Ki7.142011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC502.829011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.681011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC507.793011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki2.771011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC502.974011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.630011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC504.817011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.672011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC502.585011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki1.857011
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC502.600011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC500.967011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki0.792211
Phospholipase D1Homo sapiens (human)IC5015.500023
Phospholipase D1 Rattus norvegicus (Norway rat)IC5020.000011
Phospholipase D2Homo sapiens (human)IC5013.250012
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC500.904011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)Ki0.026237
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC501.275922
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.792211
Progesterone receptorHomo sapiens (human)IC5050.032324
Prostaglandin G/H synthase 1Homo sapiens (human)IC504.391011
Protein kinase C alpha typeHomo sapiens (human)IC5010.500022
Protein kinase C alpha typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C beta typeHomo sapiens (human)IC5010.500022
Protein kinase C beta typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C delta typeHomo sapiens (human)IC5010.500022
Protein kinase C delta typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C epsilon typeHomo sapiens (human)IC5010.500022
Protein kinase C epsilon typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C eta typeHomo sapiens (human)IC5010.500022
Protein kinase C eta typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C gamma typeHomo sapiens (human)IC5010.500022
Protein kinase C gamma typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C iota typeHomo sapiens (human)IC5010.500022
Protein kinase C theta typeHomo sapiens (human)IC5010.500022
Protein kinase C theta typeRattus norvegicus (Norway rat)IC5075.000011
Protein kinase C zeta typeHomo sapiens (human)IC5010.500022
Protein kinase C zeta typeRattus norvegicus (Norway rat)IC5075.000011
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC502.949011
Serine/threonine-protein kinase D1Homo sapiens (human)IC5010.500022
Serine/threonine-protein kinase D3Homo sapiens (human)IC5010.500022
Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)IC5030.573011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.021011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.021922
Sodium-dependent dopamine transporter Homo sapiens (human)IC501.841011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.462011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.472011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.459011
Sodium-dependent serotonin transporterHomo sapiens (human)IC502.334011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.240011
Steroid hormone receptor ERR1Homo sapiens (human)IC500.101012
Substance-K receptorHomo sapiens (human)IC503.670011
Substance-K receptorHomo sapiens (human)Ki1.223011
Substance-P receptorHomo sapiens (human)IC5015.656011
Substance-P receptorHomo sapiens (human)Ki8.540011
Thromboxane-A synthase Homo sapiens (human)IC500.916011
Transcriptional activator protein LuxRAliivibrio fischeriIC5040.000011
Tyrosine-protein kinase FynHomo sapiens (human)IC501.195011
Tyrosine-protein kinase LckHomo sapiens (human)IC508.033011
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC5020.000012

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Kd0.001011
7-dehydrocholesterol reductaseHomo sapiens (human)Kd0.001011
Angiotensin-converting enzyme 2 Homo sapiens (human)EC5051.495012
ATP-dependent translocase ABCB1Homo sapiens (human)EC5056.500011
Estrogen receptorHomo sapiens (human)EC500.723368
Estrogen receptorRattus norvegicus (Norway rat)EC50150.000012
Estrogen receptorHomo sapiens (human)Kd0.004711
Estrogen receptor betaHomo sapiens (human)EC500.980835
Estrogen receptor betaRattus norvegicus (Norway rat)EC50150.000012
Estrogen-related receptor gammaHomo sapiens (human)EC500.015011
Lysosomal acid glucosylceramidaseHomo sapiens (human)EC502.500011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC505.275012
Procathepsin LHomo sapiens (human)EC5051.495012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC5051.495012
Replicase polyprotein 1abBetacoronavirus England 1EC5051.495012
Replicase polyprotein 1abHuman coronavirus 229EEC5051.495012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC5051.495012
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC5051.495012
Spike glycoproteinBetacoronavirus England 1EC5051.495012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC5051.495012
streptokinase A precursorStreptococcus pyogenes M1 GASEC5078.086022
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC500.490011
Transmembrane protease serine 2Homo sapiens (human)EC5051.495012

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Estrogen receptorRattus norvegicus (Norway rat)A500.020011
Estrogen receptorHomo sapiens (human)Activity0.000111
Estrogen receptorHomo sapiens (human)DC500.030413
Estrogen receptor betaRattus norvegicus (Norway rat)A500.020011
Glutathione reductase, mitochondrialHomo sapiens (human)Km160.000011
heat shock protein 90, putativePlasmodium falciparum 3D7AC507.757011
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC506.320011
interferon gamma precursorHomo sapiens (human)AC5035.240011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km32.000011