Page last updated: 2024-08-05 15:01:50

aryl hydrocarbon receptor agonist

An agonist that binds to and activates aryl hydrocarbon receptors (AhRs).

ChEBI ID: 72768

Members (9)

MemberDefinitionClass
1,2-naphthoquinoneThe parent structure of the family of 1,2-naphthoquinones, in which the oxo groups of the quinone moiety are at positions 1 and 2 of the naphthalene ring. It is a metabolite of naphthalene and is found in diesel exhaust particles.1,2-naphthoquinone
2-(methylthio)benzothiazoleAn organic sulfide that is the methyl thioether of 1,3-benzothiazole-2-thiol.2-methylthio-1,3-benzothiazole
3-methylcholanthreneA pentacyclic ortho- and peri-fused polycyclic arene consisting of a dihydrocyclopenta[ij]tetraphene ring system with a methyl substituent at the 3-position.3-methylcholanthrene
alpha-naphthoflavoneAn extended flavonoid resulting from the formal fusion of a benzene ring with the h side of flavone. A synthetic compound, it is an inhibitor of aromatase (EC 1.14.14.14).alpha-naphthoflavone
beta-naphthoflavoneAn extended flavonoid resulting from the formal fusion of a benzene ring with the f side of flavone.beta-naphthoflavone
cyprodinilA member of the class of aminopyrimidine that is N-phenylpyrimidin-2-amine carrying additional cyclopropyl and methyl substituents at positions 4 and 6 respectively. A broad spectrum fungicide used to control a range of pathogens including Tapesia yallundae, Botrytis spp., Alternaria spp. and Rhynchospium secalis. Whilst it is a recognised irritant no serious human health concerns have been identified. It is moderately toxic to birds as well as most aquatic organisms and earthworms, but it is not considered toxic to honeybees.cyprodinil
mepanipyrimA member of the class of aminopyrimidines that is N-phenylpyrimidin-2-amine carrying additional methyl and 1-propynyl substituents at positions 4 and 6 respectively. A fungicide used to control a wide range of diseases including grey mould on strawberries, tomatoes and cucumabers, and scab on apples and pears.mepanipyrim
pyrimethanilA member of the class of aminopyrimidines that is N-phenylpyrimidin-2-amine carrying two additional methyl substituents at positions 4 and 6. A fungicide used to control grey mould on fruit, vegetables and ornamentals as well as leaf scab on pome fruit. Also commonly employed to control Botrytis cinerea throughout the winemaking process in grapes, must, fermenting must and wine.pyrimethanil
tranilastAn amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.tranilast

Research

Studies (9,221)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19905,825 (63.17)18.7374
1990's1,471 (15.95)18.2507
2000's990 (10.74)29.6817
2010's758 (8.22)24.3611
2020's177 (1.92)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials30 (0.30%)5.53%
Reviews201 (1.99%)6.00%
Case Studies55 (0.55%)4.05%
Observational1 (0.01%)0.25%
Other9,793 (97.15%)84.16%

Protein Targets (198)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency12.064713
15-lipoxygenase, partialHomo sapiens (human)Potency25.118911
67.9K proteinVaccinia virusPotency8.912511
activating transcription factor 6Homo sapiens (human)Potency21.470823
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency31.342414
alpha-galactosidaseHomo sapiens (human)Potency7.079511
AR proteinHomo sapiens (human)Potency27.7146930
aryl hydrocarbon receptorHomo sapiens (human)Potency24.6741314
arylsulfatase AHomo sapiens (human)Potency6.745611
ATAD5 protein, partialHomo sapiens (human)Potency6.200244
Ataxin-2Homo sapiens (human)Potency1.361223
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency21.773835
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.567624
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency9.528311
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency3.689811
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency64.467912
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency11.677312
caspase-3Homo sapiens (human)Potency11.677312
Cellular tumor antigen p53Homo sapiens (human)Potency18.006924
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency18.070723
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.970315
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency28.183811
Chain A, Beta-lactamaseEscherichia coli K-12Potency14.407422
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, HADH2 proteinHomo sapiens (human)Potency26.759424
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency23.877022
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency3.539711
Chain B, HADH2 proteinHomo sapiens (human)Potency26.759424
chromobox protein homolog 1Homo sapiens (human)Potency0.006011
cytochrome P450 2C19 precursorHomo sapiens (human)Potency1.995311
cytochrome P450 2C9 precursorHomo sapiens (human)Potency7.943311
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.589311
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.294724
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency9.861516
DNA polymerase betaHomo sapiens (human)Potency31.622811
dopamine D1 receptorHomo sapiens (human)Potency29.092911
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.6359936
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency2.730611
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency8.6711929
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.348116
farnesoid X nuclear receptorHomo sapiens (human)Potency34.631223
GABA theta subunitRattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.294712
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.294712
gemininHomo sapiens (human)Potency29.713612
GLI family zinc finger 3Homo sapiens (human)Potency32.250338
glp-1 receptor, partialHomo sapiens (human)Potency1.584911
glucocerebrosidaseHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency42.116035
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency13.169817
Guanine nucleotide-binding protein GHomo sapiens (human)Potency56.234111
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency2.074923
heat shock protein beta-1Homo sapiens (human)Potency37.014324
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.943313
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.183811
histone deacetylase 9 isoform 3Homo sapiens (human)Potency25.587527
Histone H2A.xCricetulus griseus (Chinese hamster)Potency73.632823
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency15.649812
hypothetical protein, conservedTrypanosoma bruceiPotency31.622811
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.943322
Integrin alpha-IIbHomo sapiens (human)Potency10.000011
Integrin beta-3Homo sapiens (human)Potency10.000011
lamin isoform A-delta10Homo sapiens (human)Potency0.022411
lethal factor (plasmid)Bacillus anthracis str. A2012Potency25.118911
LuciferasePhotinus pyralis (common eastern firefly)Potency13.475349
M-phase phosphoprotein 8Homo sapiens (human)Potency0.199511
Microtubule-associated protein tauHomo sapiens (human)Potency13.758825
mitogen-activated protein kinase 1Homo sapiens (human)Potency12.057023
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.125911
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency17.647614
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.589311
NFKB1 protein, partialHomo sapiens (human)Potency28.183822
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency5.011911
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency0.534913
Nrf2Homo sapiens (human)Potency0.631011
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.5086414
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency24.600711
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency3.398126
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.5961314
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency19.952611
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency35.481311
ParkinHomo sapiens (human)Potency13.081622
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency7.568611
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency23.571822
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency49.897633
phosphopantetheinyl transferaseBacillus subtilisPotency32.535213
plasminogen precursorMus musculus (house mouse)Potency7.079511
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency7.079511
pregnane X nuclear receptorHomo sapiens (human)Potency30.416727
pregnane X receptorRattus norvegicus (Norway rat)Potency27.829812
progesterone receptorHomo sapiens (human)Potency27.474812
pyruvate kinaseLeishmania mexicana mexicanaPotency12.589322
pyruvate kinase PKM isoform aHomo sapiens (human)Potency12.589322
pyruvate kinase PKM isoform bHomo sapiens (human)Potency19.952622
RAR-related orphan receptor gammaMus musculus (house mouse)Potency5.264329
ras-related protein Rab-9AHomo sapiens (human)Potency0.361113
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency11.5541315
retinoid X nuclear receptor alphaHomo sapiens (human)Potency38.406722
SMAD family member 2Homo sapiens (human)Potency17.185412
SMAD family member 3Homo sapiens (human)Potency17.185412
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency0.492912
TDP1 proteinHomo sapiens (human)Potency16.579526
thioredoxin glutathione reductaseSchistosoma mansoniPotency11.220211
ThrombopoietinHomo sapiens (human)Potency10.000022
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.207427
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency42.519844
thyroid stimulating hormone receptorHomo sapiens (human)Potency28.303744
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.079511
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.079511
USP1 protein, partialHomo sapiens (human)Potency76.110412
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency38.479224
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency61.644811
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency13.169817

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseHomo sapiens (human)IC5022.683011
AcetylcholinesteraseHomo sapiens (human)Ki0.320022
Adenosine receptor A1Bos taurus (cattle)IC503.000011
Adenosine receptor A1Homo sapiens (human)IC501.132511
Adenosine receptor A1Homo sapiens (human)Ki0.660611
Adenosine receptor A3Homo sapiens (human)IC505.544011
Adenosine receptor A3Homo sapiens (human)Ki3.134011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC5029.650011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki29.405011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC505.544011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki3.134011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC505.544011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki3.134011
AromataseHomo sapiens (human)IC501.035022
AromataseHomo sapiens (human)Ki0.020011
Aryl hydrocarbon receptorMus musculus (house mouse)IC500.025011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent translocase ABCB1Homo sapiens (human)IC5024.600011
Bile salt export pumpHomo sapiens (human)IC5041.500011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC504.270024
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Carboxylic ester hydrolase Sus scrofa (pig)IC500.047811
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC502.303411
CholinesteraseHomo sapiens (human)Ki1.646035
Coagulation factor XIIHomo sapiens (human)Ki1.873313
Cytochrome P450 1A1Homo sapiens (human)IC502.36652627
Cytochrome P450 1A1Homo sapiens (human)Ki0.045011
Cytochrome P450 1A2Homo sapiens (human)IC501.98523941
Cytochrome P450 1A2Homo sapiens (human)Ki0.020011
Cytochrome P450 1B1Homo sapiens (human)IC5010.87873434
Cytochrome P450 1B1Homo sapiens (human)Ki0.016011
Cytochrome P450 2A6Homo sapiens (human)IC5025.000012
Cytochrome P450 2B6Homo sapiens (human)IC5019.000012
Cytochrome P450 2C19Homo sapiens (human)IC5015.000044
Cytochrome P450 2C9 Homo sapiens (human)IC5015.000044
Cytochrome P450 2D6Homo sapiens (human)IC5013.333366
Cytochrome P450 3A4Homo sapiens (human)IC5013.333366
Cytochrome P450 3A6Oryctolagus cuniculus (rabbit)Ki80.100011
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)IC5010.610011
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC504.980011
GABA theta subunitRattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki1.480011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki1.480011
Genome polyprotein Human rhinovirus sp.IC508.200011
Hematopoietic prostaglandin D synthaseHomo sapiens (human)IC5011.600022
Histamine H3 receptorCavia porcellus (domestic guinea pig)IC5020.000012
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC507.100022
Liver carboxylesterase 1Homo sapiens (human)Ki1.637524
Mitogen-activated protein kinase 3 Homo sapiens (human)IC505.466711
Multidrug resistance-associated protein 1 Homo sapiens (human)IC5011.300011
Multidrug resistance-associated protein 4Homo sapiens (human)IC501.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC5025.000011
PapainCarica papaya (papaya)IC50120.000011
Protein skinhead-1Caenorhabditis elegansIC50100.000011
Receptor-type tyrosine-protein phosphatase CHomo sapiens (human)IC503.000011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC500.010011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC5029.650011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki29.405011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.050011
Substance-K receptorHomo sapiens (human)IC505.847111
Substance-K receptorHomo sapiens (human)Ki1.949011
TatHuman immunodeficiency virus 1IC5030.461011
Thromboxane-A synthase Homo sapiens (human)IC506.760811
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC50125.946512
Transient receptor potential cation channel subfamily V member 2Homo sapiens (human)IC5010.000011
Tyrosine-protein kinase FynHomo sapiens (human)IC5013.846012
Tyrosine-protein kinase LckHomo sapiens (human)IC5055.452011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC501.640011
Tyrosine-protein phosphatase non-receptor type 22Homo sapiens (human)IC501.100011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50115.400015
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50115.400015
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50115.400015
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50115.400015
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50115.400015
VifHuman immunodeficiency virus 1IC5010.610011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC5020.000012

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aryl hydrocarbon receptorHomo sapiens (human)EC500.939755
Cytochrome P450 1A1Homo sapiens (human)EC502.500022
Cytochrome P450 1B1Homo sapiens (human)EC5026.700033
recombinase AMycobacterium tuberculosis H37RvEC509.135522

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aryl hydrocarbon receptorHomo sapiens (human)Concentration100.000011
Cytochrome P450 1B1Homo sapiens (human)Ks0.700011
LMP1 [Human herpesvirus 4]human gammaherpesvirus 4 (Epstein-Barr virus)AC508.533011
MSHDrosophila melanogaster (fruit fly)AC500.594011
NADHomo sapiens (human)CD0.012011
NAD(P)H dehydrogenase [quinone] 1Mus musculus (house mouse)CD0.028011
PAX8Homo sapiens (human)AC502.140033
Quinone oxidoreductaseMus musculus (house mouse)Activity0.146011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC5010.376022