Page last updated: 2024-08-05 14:53:32

tropomyosin-related kinase B receptor agonist

An agonist that binds to and deactivates the tropomyosin-related kinase B (TrkB) receptor, the main signaling receptor of the neurotrophin brain-derived neurotrophic factor (BDNF).

ChEBI ID: 140489

Members (4)

MemberDefinitionClass
7,8-dihydroxyflavoneA dihydroxyflavone that is flavone substituted by hydroxy groups at positions 7 and 8. A dihydroxyflavone that is flavone substituted by hydroxy groups at positions 7 and 8. A naturally occurring flavonoid produced by several plants, including the weed Tridax procumbens (coalbuttons or tridax daisy) and the tree Godmania aesculifolia, In animal models, it has shown efficacy against several diseases of the nervous system, including Alzheimer's, Parkinson's, and Huntington's.7,8-dihydroxyflavone
amitriptylineAn organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.amitriptyline
diosmetinA monomethoxyflavone that is the 4'-methyl ether derivative of luteolin. It is a natural product isolated from citrus fruits which exhibits a range of pharmacological activities.diosmetin
n-acetylserotoninAn N-acylserotonin resulting from the formal condensation of the primary amino group of serotonin with the carboxy group of acetic acid.N-acetylserotonin

Research

Studies (6,920)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19903,522 (50.90)18.7374
1990's1,040 (15.03)18.2507
2000's954 (13.79)29.6817
2010's1,072 (15.49)24.3611
2020's332 (4.80)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,381 (18.34%)5.53%
Reviews417 (5.54%)6.00%
Case Studies872 (11.58%)4.05%
Observational13 (0.17%)0.25%
Other4,845 (64.36%)84.16%

Protein Targets (162)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency7.191212
15-lipoxygenase, partialHomo sapiens (human)Potency5.011911
67.9K proteinVaccinia virusPotency27.005022
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.895912
arylsulfatase AHomo sapiens (human)Potency3.013111
Ataxin-2Homo sapiens (human)Potency12.589311
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency13.091811
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.003222
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589322
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency21.845613
Chain A, HADH2 proteinHomo sapiens (human)Potency8.971622
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency9.106312
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency6.190412
Chain B, HADH2 proteinHomo sapiens (human)Potency8.971622
chromobox protein homolog 1Homo sapiens (human)Potency25.118911
cytochrome P450 2D6Homo sapiens (human)Potency9.522111
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency21.201013
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency24.291026
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.091611
D(1A) dopamine receptorHomo sapiens (human)Potency0.690622
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency25.118911
DNA polymerase kappa isoform 1Homo sapiens (human)Potency8.912511
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.849311
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency5.669712
EWS/FLI fusion proteinHomo sapiens (human)Potency10.657944
GABA theta subunitRattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency24.291013
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency24.291013
gemininHomo sapiens (human)Potency0.194622
GLS proteinHomo sapiens (human)Potency3.530523
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency18.938916
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency15.848911
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
Interferon betaHomo sapiens (human)Potency11.708613
Microtubule-associated protein tauHomo sapiens (human)Potency33.205823
mitogen-activated protein kinase 1Homo sapiens (human)Potency2.511911
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.174922
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.000011
NFKB1 protein, partialHomo sapiens (human)Potency5.011922
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency1.933111
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency22.740622
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency18.938913
PPM1D proteinHomo sapiens (human)Potency11.708612
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.689222
survival motor neuron protein isoform dHomo sapiens (human)Potency35.481311
TDP1 proteinHomo sapiens (human)Potency19.849623
thioredoxin reductaseRattus norvegicus (Norway rat)Potency24.688012
USP1 protein, partialHomo sapiens (human)Potency48.022412
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency22.478655

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.020022
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.141011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.020022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki1.141011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.015011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.004411
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.070011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.045011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.006011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.003211
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.006011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.003211
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.140011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC500.044011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.065011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5016.900012
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC500.044011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.023011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.022011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.000011
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.105011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.052011
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.175522
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.132011
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.004022
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.003711
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.029522
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.008611
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5017.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)IC5017.000011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5017.589411
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki14.410611
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Aurora kinase BHomo sapiens (human)IC503.860011
Bile salt export pumpHomo sapiens (human)IC50134.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5091.500022
Cytochrome P450 1A1Homo sapiens (human)IC500.140011
Cytochrome P450 1A1Homo sapiens (human)Ki0.089011
Cytochrome P450 1A2Homo sapiens (human)IC502.437011
Cytochrome P450 1B1Homo sapiens (human)IC500.029011
Cytochrome P450 1B1Homo sapiens (human)Ki0.016022
D(1A) dopamine receptorHomo sapiens (human)IC500.355011
D(1A) dopamine receptorHomo sapiens (human)Ki0.133522
D(1B) dopamine receptorHomo sapiens (human)Ki0.170011
D(2) dopamine receptorHomo sapiens (human)IC501.009011
D(2) dopamine receptorHomo sapiens (human)Ki0.266022
D(3) dopamine receptorHomo sapiens (human)IC500.182011
D(3) dopamine receptorHomo sapiens (human)Ki0.134022
High affinity nerve growth factor receptorHomo sapiens (human)IC5060.000011
Histamine H1 receptorHomo sapiens (human)IC500.004811
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.000012
Histamine H1 receptorHomo sapiens (human)Ki0.000822
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC500.660011
Histamine H2 receptorHomo sapiens (human)IC500.730011
Histamine H2 receptorHomo sapiens (human)Ki0.718011
Histamine H3 receptorHomo sapiens (human)Ki1.000011
Inhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)IC509.820011
Inositol hexakisphosphate kinase 2Homo sapiens (human)IC500.900011
Inositol polyphosphate multikinaseHomo sapiens (human)IC507.200011
large T antigenBetapolyomavirus macacaeIC5021.670011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC5027.900011
Mitogen-activated protein kinase 10Homo sapiens (human)IC5025.900012
Mitogen-activated protein kinase 14Homo sapiens (human)IC5025.900012
Multidrug resistance-associated protein 1 Homo sapiens (human)IC503.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.011011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.300014
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.002711
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.081011
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.029011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.026011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.005411
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.005311
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.000711
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.008011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.005811
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5017.589411
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki14.410611
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)IC5093.600011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC507.98351414
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki14.410611
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC509.900011
Sepiapterin reductaseHomo sapiens (human)IC505.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.031011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.433011
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC5011.550022
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5010.800022
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC5020.000011
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC509.333333
Sodium-dependent dopamine transporter Homo sapiens (human)IC5012.589211
Sodium-dependent dopamine transporter Homo sapiens (human)Ki6.203011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.032422
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.177522
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.275622
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.028456
Solute carrier family 22 member 1 Homo sapiens (human)IC5016.900011
Telomerase reverse transcriptaseHomo sapiens (human)IC5036.000011
TyrosinaseMus musculus (house mouse)IC50311.000011
TyrosinaseMus musculus (house mouse)Ki240.000011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5011.600011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC5011.600011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC5011.600011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC5011.600011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5012.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminRattus norvegicus (Norway rat)Kd134.000011
BDNF/NT-3 growth factors receptorHomo sapiens (human)Kd0.165022
High affinity nerve growth factor receptorHomo sapiens (human)EC5086.000011
High affinity nerve growth factor receptorHomo sapiens (human)Kd2,050.000044
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)EC5086.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Catechol O-methyltransferaseRattus norvegicus (Norway rat)Km3.240022
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.000512
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km267.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km110.000023