Page last updated: 2024-11-07

3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan

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Description

3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan: structure given in first source; substance P and neurokinin receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132837
CHEMBL ID22870
SCHEMBL ID3682000
MeSH IDM0228251

Synonyms (61)

Synonym
BIDD:GT0377
148451-96-1
n-acetyl-l-trytophan 3,5-bis(trifluoromethyl)benzyl ester
MLS002172463
smr001254094
LOPAC0_000028
EU-0100028
n-acetyl-l-tryptophan 3,5-bis(trifluoromethyl)benzyl ester, >=99% (tlc), powder
tocris-0868
lopac-a-5330
NCGC00024832-01
NCGC00015066-01
l-732,138
n-acetyltryptophan 3,5-bis(trifluoromethyl)benzyl ester
l 732138
[3,5-bis(trifluoromethyl)phenyl]methyl (2s)-2-acetamido-3-(1h-indol-3-yl)propanoate
l732138
chembl22870 ,
bdbm21016
n-acetyl-l-tryptophan-3,5-bistrifluoromethylbenzyl ester
3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan
n-acetyl-l-trp-3,5-bistrifluoromethylbenzyl ester
l-tryptophan, n-acetyl-, (3,5-bis(trifluoromethyl)phenyl)methyl ester
3,5-bis(tfm)bz nactrp
NCGC00024832-03
NCGC00024832-02
A 5330
NCGC00024832-04
l-732138
HMS3260E17
CCG-204124
HMS2234A11
LP00028
AKOS015898307
SCHEMBL3682000
NCGC00260713-01
tox21_500028
DTXSID20163989
mfcd00237267
SR-01000597431-1
sr-01000597431
n-acetyl-l-tryptophan 3,5-bis(trifluoromethyl) benzyl ester
gtpl9461
SR-01000075194-1
sr-01000075194
(s)-3,5-bis(trifluoromethyl)benzyl 2-acetamido-3-(1h-indol-3-yl)propanoate
ac-trp-3,5-bis(trifluoromethyl)benzylester
ac-trp-3,5-bis(trifluoromethyl)benzyl ester
3,5-bis(trifluoromethyl)benzyl acetyl-l-tryptophanate
BS-15443
3,5-bis(trifluoromethyl)benzylacetyl-l-tryptophanate
S0772
l-tryptophan, n-acetyl-, [3,5-bis(trifluoromethyl)phenyl]methyl ester
n-acetyl-l-tryptophan 3,5-bis(trifluoromethyl)benzylester
SDCCGSBI-0050017.P002
NCGC00024832-05
HY-101249
CS-0021036
D81775
GLXC-15006
byyqyxvawxayqc-ibgzpjmesa-n
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (78)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency18.44690.003245.467312,589.2998AID1705; AID2517
Chain A, Beta-lactamaseEscherichia coli K-12Potency25.11890.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency15.84895.623417.292931.6228AID2323
Chain A, CruzipainTrypanosoma cruziPotency17.90080.002014.677939.8107AID1476
endonuclease IVEscherichia coliPotency22.38720.707912.432431.6228AID1708
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency39.81070.100020.879379.4328AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency29.88160.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency10.00000.02827.055915.8489AID895; AID928
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1468
ThrombopoietinHomo sapiens (human)Potency12.58930.02517.304831.6228AID917; AID918
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency28.18380.28189.721235.4813AID2326
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency36.04150.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency22.38720.540617.639296.1227AID2364; AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency39.81070.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency25.11890.316212.443531.6228AID902
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.94330.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.58930.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency28.18383.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency12.58930.01789.637444.6684AID588834
DNA polymerase betaHomo sapiens (human)Potency15.84890.022421.010289.1251AID485314
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency56.23410.425612.059128.1838AID504891
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency15.84890.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency28.18380.00798.23321,122.0200AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency42.28410.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.94330.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency56.23410.177824.735279.4328AID488949
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency10.73620.891312.067628.1838AID1459; AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency1.58490.015812.3113615.5000AID1461
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.58930.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency6.30961.000010.475628.1838AID901
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency44.66843.981146.7448112.2020AID720708
GABA theta subunitRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00300.77706.0000AID145814
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00030.30952.3000AID145814
Neuronal acetylcholine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00300.03470.1000AID145814
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00030.32092.3000AID145814
Neuronal acetylcholine receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00200.02680.1000AID145814
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00300.88696.0000AID145814
Substance-P receptorRattus norvegicus (Norway rat)IC50 (µMol)38.71850.00010.19930.3981AID145802; AID391167; AID422080; AID452779; AID592527
Substance-P receptorRattus norvegicus (Norway rat)Ki0.11480.00070.12981.0000AID1798027; AID1798029; AID320356; AID391167; AID422080; AID452779; AID592527
Neuromedin-K receptorRattus norvegicus (Norway rat)IC50 (µMol)5.00000.01100.01100.0110AID145954
Substance-K receptorRattus norvegicus (Norway rat)IC50 (µMol)0.39810.20000.29910.3981AID497528
Substance-K receptorRattus norvegicus (Norway rat)Ki0.13400.00050.06870.1340AID497528
Neuronal acetylcholine receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00300.03470.1000AID145814
Substance-K receptorHomo sapiens (human)IC50 (µMol)5.00000.00013.12109.5530AID145472; AID145814
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.02880.00000.09526.8130AID144536; AID145784; AID147677; AID208267; AID208268; AID208269; AID208271; AID208591; AID288854; AID391166; AID422079; AID452778; AID497529; AID592526
Substance-P receptorHomo sapiens (human)Ki0.02990.00000.79368.7470AID1798027; AID288854; AID320355; AID391166; AID422079; AID452778; AID497529; AID592526
Neuromedin-K receptorHomo sapiens (human)IC50 (µMol)5.00000.00100.28822.9900AID145954
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00150.00010.729810.0000AID592526
Delta-type opioid receptorMus musculus (house mouse)Ki0.00070.00000.53939.4000AID592526
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.08820.00000.38458.6000AID1798027; AID1798029
Delta-type opioid receptorHomo sapiens (human)Ki0.13400.00000.59789.9300AID1798029
Neuronal acetylcholine receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00200.69046.0000AID145814
Neuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00240.03010.1000AID145814
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.39810.00020.660310.0000AID452779
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.13400.00000.27869.0000AID452779
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00301.69437.0795AID145814
Neuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00300.03470.1000AID145814
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (90)

Processvia Protein(s)Taxonomy
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwayNeuromedin-K receptorHomo sapiens (human)
positive regulation of heart rateNeuromedin-K receptorHomo sapiens (human)
response to estradiolNeuromedin-K receptorHomo sapiens (human)
regulation of dopamine metabolic processNeuromedin-K receptorHomo sapiens (human)
response to cocaineNeuromedin-K receptorHomo sapiens (human)
positive regulation of blood pressureNeuromedin-K receptorHomo sapiens (human)
regulation of feeding behaviorNeuromedin-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionNeuromedin-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilityNeuromedin-K receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingNeuromedin-K receptorHomo sapiens (human)
tachykinin receptor activityNeuromedin-K receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneSubstance-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
dendrite membraneNeuromedin-K receptorHomo sapiens (human)
neuronal cell body membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

Assay IDTitleYearJournalArticle
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1798027Radioligand Labeled Binding Assay from Article 10.1021/jm070332f: \\A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Recep2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID1798029Radioligand Labeled Binding Assay from Article 10.1021/jm061369n: \\Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.\\2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID592527Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID288863Antagonist activity at NK1 receptor in Hartley guinea pig isolated ileum assessed as inhibition of substance P-induced muscle contraction2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID497528Displacement of [3H]substance P frome rat NK2 receptor2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
AID422079Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
AID391167Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane by liquid scintillation counting2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID288854Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID391175Antagonist activity at NK1 receptor in Hartley guinea pig ileum longitudinal muscle with myenteric plexus assessed as inhibition of substance P-induced muscle contraction in presence of naloxone2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID497529Displacement of [3H]substance P frome human NK1 receptor2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
AID592526Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
AID452779Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membranes2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
AID592528Selectivity ratio of Ki for rat NK1 receptor to Ki for human NK1 receptor2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
AID320356Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID208271Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID208268Binding affinity at human Tachykinin receptor 1 expressed in CHO cells by [125 I]Trp8-substance P displacement.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.
AID145784Binding affinity towards cloned neurokinin 1 receptor, based on the displacement of [125I]-labeled substance P1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID422151Antagonist activity at NK1 receptor in guinea pig ileum assessed as inhibition of substance P-induced muscle contraction in presence of opioid receptor inhibitor naloxone2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
AID208591Binding affinity was measured against the Tachykinin receptor 1 in CHO-expressed hNK1 using [125I]SP.1998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.
AID144536Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
AID391168Ratio of Ki for human NK1 receptor to Ki for rat NK1 receptor2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID145814Binding affinity to the NK2 receptor assayed by displacement of [125I]-Neurokinin A1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID452778Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membranes2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
AID145472Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
L-tryptophan urea amides as NK1/NK2 dual antagonists.
AID320355Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID391166Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID77594% inhibition against substance P induced extravasation in the guinea pig at an oral dose of 30 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID147677Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
L-tryptophan urea amides as NK1/NK2 dual antagonists.
AID229517Ratio of IC50 value against hNK1 receptor to that of Q165A receptor.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID452788Antagonist activity at NK1 receptor in guinea pig ileum assessed as inhibition of substance P-induced muscle contraction in presence of naloxone2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
AID592531Antagonist activity at NK1 receptor in guinea pig ileum assessed as inhibition of substance P-induced muscle contraction2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
AID1323835Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID422081Selectivity ratio, Ki for human NK1 receptor to Ki for rat NK1 receptor2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
AID208269Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID145802The inhibitory concentration against rat neurokinin-1 receptor1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID76844Inhibitory dose against substance P induced extravasation in the guinea pig1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID497538Antagonist activity at NK1 receptor in guinea pig ileum assessed as inhibition of substance P-induced muscle contraction2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
AID1323834Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID320364Antagonist activity at NK1 receptor in Hartley guinea pig isolated ileum assessed as inhibition of substance P-induced muscle contraction2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID320359Ratio of Ki for human NK1 over Ki for rat NK12008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
AID422080Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
AID145954Affinity to NK3 receptors assayed by displacement of [125I]-Bolton-Hunter labeled eledoisin radioligand1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID208267Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1346354Rat NK1 receptor (Tachykinin receptors)1994The Journal of biological chemistry, Mar-04, Volume: 269, Issue:9
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.
AID1346346Human NK1 receptor (Tachykinin receptors)1994The Journal of biological chemistry, Mar-04, Volume: 269, Issue:9
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (74)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (13.51)18.2507
2000's32 (43.24)29.6817
2010's26 (35.14)24.3611
2020's6 (8.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.41

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.41 (24.57)
Research Supply Index4.33 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other75 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]