Page last updated: 2024-11-04

6-chloromelatonin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID1858
CHEMBL ID34730
CHEBI ID109545
SCHEMBL ID677518
SCHEMBL ID677517
MeSH IDM0082031

Synonyms (61)

Synonym
MLS002153444
smr001230810
melatonin, 6-chloro
n-[2-(6-chloro-5-methoxy-1h-indol-3-yl)-ethyl]-acetamide(6-chloromelatonin)
bdbm50043289
n-[2-(6-chloro-5-methoxy-1h-indol-3-yl)-ethyl]-acetamide
HMS3266A08
BRD-K34663752-001-02-6
6-cl-melatonin
gtpl1346
6-cl-mlt
brn 0410191
acetamide, n-(2-(6-chloro-5-methoxy-1h-indol-3-yl)ethyl)-
n-(2-(6-chloro-5-methoxy-1h-indol-3-yl)ethyl)acetamide
EU-0100178
NCGC00015203-01
tocris-0443
lopac-c-0331
NCGC00024593-01
LOPAC0_000178
PDSP1_001786
PDSP2_001769
NCGC00024593-04
6-chloromelatonin
NCGC00024593-03
NCGC00024593-02
NCGC00015203-03
CHEBI:109545
C 0331
n-acetyl-6-chloro-5-methoxytryptamine
NCGC00015203-06
CHEMBL34730 ,
L000082
63762-74-3
n-[2-(6-chloro-5-methoxy-1h-indol-3-yl)ethyl]acetamide
HMS3260D17
CCG-204273
HMS2234G13
NCGC00015203-05
NCGC00015203-04
NCGC00015203-02
LP00178
HMS3374G08
SCHEMBL677518
SCHEMBL677517
tox21_500178
NCGC00260863-01
n-[2-(5-methoxy-6-chloroindol-3-yl)ethyl]acetamide
LUINDDOUWHRIPW-UHFFFAOYSA-N
n-[2-(6-chloro-5-methoxyindol-3-yl)ethyl]acetamide
AKOS024458157
DTXSID30213202
SR-01000075735-3
sr-01000075735
SR-01000075735-1
HMS3675M07
Q27074008
HMS3411M07
SDCCGSBI-0050166.P002
HY-100940
CS-0020611
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
acetamidesCompounds with the general formula RNHC(=O)CH3.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (39)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
endonuclease IVEscherichia coliPotency4.46680.707912.432431.6228AID1708
ATAD5 protein, partialHomo sapiens (human)Potency16.35350.004110.890331.5287AID504466
NFKB1 protein, partialHomo sapiens (human)Potency3.16230.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency0.31620.35487.935539.8107AID624146
ThrombopoietinHomo sapiens (human)Potency25.11890.02517.304831.6228AID917; AID918
Smad3Homo sapiens (human)Potency5.62340.00527.809829.0929AID588855
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.58930.00137.762544.6684AID914; AID915
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency13.35100.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00010.540617.639296.1227AID2364; AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency39.81070.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency5.01190.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency14.97630.00636.904339.8107AID883
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID995
gemininHomo sapiens (human)Potency0.56230.004611.374133.4983AID624297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency4.45770.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.00100.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency14.97630.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency31.62280.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.25620.060110.745337.9330AID485368
[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)
Melatonin receptor type 1AHomo sapiens (human)IC50 (µMol)0.00240.00000.06401.0200AID107558; AID107559; AID165366
Melatonin receptor type 1AHomo sapiens (human)Ki0.00470.00000.27359.1000AID107564; AID107565; AID107567; AID1138127; AID1527859
Melatonin receptor type 1BHomo sapiens (human)IC50 (µMol)0.00240.00000.34894.0000AID107558; AID107559; AID165366
Melatonin receptor type 1BHomo sapiens (human)Ki0.00090.00000.16289.1000AID107564; AID107565; AID107567; AID1138128; AID1527860
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1AHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
mating behaviorMelatonin receptor type 1AHomo sapiens (human)
circadian rhythmMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1BHomo sapiens (human)
chemical synaptic transmissionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cGMP-mediated signalingMelatonin receptor type 1BHomo sapiens (human)
glucose homeostasisMelatonin receptor type 1BHomo sapiens (human)
camera-type eye developmentMelatonin receptor type 1BHomo sapiens (human)
negative regulation of neuron apoptotic processMelatonin receptor type 1BHomo sapiens (human)
negative regulation of vasoconstrictionMelatonin receptor type 1BHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, non-REM sleepMelatonin receptor type 1BHomo sapiens (human)
negative regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationMelatonin receptor type 1BHomo sapiens (human)
negative regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
positive regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
regulation of neuronal action potentialMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1BHomo 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)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protein bindingMelatonin receptor type 1AHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1AHomo sapiens (human)
hormone bindingMelatonin receptor type 1AHomo sapiens (human)
organic cyclic compound bindingMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1AHomo sapiens (human)
protein bindingMelatonin receptor type 1BHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1BHomo 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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneMelatonin receptor type 1AHomo sapiens (human)
receptor complexMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
synapseMelatonin receptor type 1BHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
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)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (73)

Assay IDTitleYearJournalArticle
AID227391Inhibition of forskolin stimulated cAMP accumulation and represented as cAMP index which is the ratio of percent inhibition to percent inhibition of melatonin1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
AID107400Negative logarithm of relative affinity (pRA) towards melatonin receptor (relative to N-acetyl-5-methoxytryptamine (aMT))1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.
AID107565Binding affinity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as labelled ligand1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID107876Relative Intrinsic activity evaluated on [35S]GTP-gamma-S, binding in NIH3T3 cells stably transfected with human Melatonin receptor type 1A2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.
AID227388GTPgammaS index is the ratio of the IC50 of compound with GTP and without GTP to the IC50 of melatonin with GTP and without GTP1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID165408Relative potency of inhibition of calcium-dependent release of [3H]dopamine from rabbit retina caused by 2-[125I]iodomelatonin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
AID227389GTPgammaS index is the ratio of the IC50 of compound with GTP and without GTP to the IC50 of melatonin with GTP and without GTP1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
AID166149Inhibition of spontaneous firing activity of single cortical neurons in the rabbit parietal cortex model at 1 x 10 e-6 M (agonist)1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
AID107545Relative binding affinity to chicken retinal membranes compared to 2-[125I]iodomelatonin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
AID107548Compound was tested in vivo for its activity against melatonin receptor in Syrian hamster gonadal regression model; Agonist1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
AID107558Inhibitory activity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as labelled ligand1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
AID107567Inhibition of 2-[125I]iodomelatonin binding to melatonin receptor in quail brain as 1/Ka1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
AID227179Activity considered from GTP-gamma-S index and cAMP index; A = agonist1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
AID1123745Antiovulatory activity in Sprague-Dawley rat assessed as blockage of luteinizing hormone surge by measuring reduction in ovulation at 5 mg/kg, po by microscopic analysis1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues.
AID1527859Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constant2020European journal of medicinal chemistry, Jan-01, Volume: 185Indole-based melatonin analogues: Synthetic approaches and biological activity.
AID1138128Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in African green monkey COS7 cells2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID107559Inhibitory activity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as radiolabeled ligand1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID230719Ratio of the IC50 of compound to the IC50 of melatonin1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
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.
AID1123744Antiovulatory activity in Sprague-Dawley rat assessed as blockage of luteinizing hormone surge by measuring reduction in ovulation at 4 mg/kg, iv by microscopic analysis1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues.
AID227033Activity considered from GTP-gamma-S and cAMP index values; A = agonist1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID1123754Half life in serum (unknown origin) after first 2 hrs post iv dose1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues.
AID227390Inhibition of forskolin stimulated cAMP accumulation and represented as cAMP index which is the ratio of percent inhibition to percent inhibition of melatonin1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID107564Binding affinity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin (100 pM) as labelled ligand1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.
AID107563Inhibition of 2-[125I]iodomelatonin binding to melatonin receptor in quail brain1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
AID1138140Selectivity ratio of Ki for human recombinant MT1 receptor to Ki for human recombinant MT2 receptor2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID107543Binding affinity to compete for 2-[125I]iodomelatonin binding to chicken retinal membranes1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
AID230718Relative binding to melatonin receptor compared to melatonin, ratio of IC501997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
AID107568Compound was tested in vivo for its activity against melatonin receptor in rabbit parietal cortex model; Agonist1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
AID165366Inhibition of 2-[125I]iodomelatonin stimulated calcium dependent dopamine release from the rabbit retina.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
AID1138127Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID1527860Binding affinity to MT2 receptor (unknown origin) assessed as inhibition constant2020European journal of medicinal chemistry, Jan-01, Volume: 185Indole-based melatonin analogues: Synthetic approaches and biological activity.
AID108040Relative Intrinsic activity evaluated on [35S]GTP-gamma-S, binding in NIH3T3 cells stably transfected with human Melatonin receptor type 1B2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.
AID1123749Melatonin-like activity in tadpole by blanching test1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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 SIRPĪ±-CD47 interaction inhibitors.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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 SIRPĪ±-CD47 interaction inhibitors.
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 SIRPĪ±-CD47 interaction inhibitors.
AID1346274Human MT2 receptor (Melatonin receptors)2003Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 367, Issue:6
New selective ligands of human cloned melatonin MT1 and MT2 receptors.
AID1346274Human MT2 receptor (Melatonin receptors)1998The Journal of pharmacology and experimental therapeutics, Jun, Volume: 285, Issue:3
GR196429: a nonindolic agonist at high-affinity melatonin receptors.
AID1346220Human MT1 receptor (Melatonin receptors)1998The Journal of pharmacology and experimental therapeutics, Jun, Volume: 285, Issue:3
GR196429: a nonindolic agonist at high-affinity melatonin receptors.
AID1346220Human MT1 receptor (Melatonin receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 355, Issue:3
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
AID1346274Human MT2 receptor (Melatonin receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 355, Issue:3
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
AID1346220Human MT1 receptor (Melatonin receptors)1985The Journal of pharmacology and experimental therapeutics, Aug, Volume: 234, Issue:2
Characterization of a retinal melatonin receptor.
AID1346274Human MT2 receptor (Melatonin receptors)1985The Journal of pharmacology and experimental therapeutics, Aug, Volume: 234, Issue:2
Characterization of a retinal melatonin receptor.
AID1346220Human MT1 receptor (Melatonin receptors)2003Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 367, Issue:6
New selective ligands of human cloned melatonin MT1 and MT2 receptors.
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 (60)

TimeframeStudies, This Drug (%)All Drugs %
pre-199010 (16.67)18.7374
1990's20 (33.33)18.2507
2000's15 (25.00)29.6817
2010's9 (15.00)24.3611
2020's6 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.46

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 Index10.46 (24.57)
Research Supply Index4.14 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (3.23%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other60 (96.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]