Page last updated: 2024-11-11

3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer

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

Cross-References

ID SourceID
PubMed CID6604724
CHEMBL ID58033
CHEBI ID107647
SCHEMBL ID10804846
MeSH IDM0329055

Synonyms (61)

Synonym
BRD-K53532120-001-02-4
LOPAC0_001266
BIO1_000902
tocris-0496
tocris-0471
BIO1_001391
BIO2_000231
tocris-0495
BIO2_000711
NCGC00024605-02
NCGC00024605-03
NCGC00024605-01
BIO1_000413
BSPBIO_001511
IDI1_033981
NCGC00024605-06
NCGC00024605-08
NCGC00024605-09
NCGC00024605-07
KBIO2_002799
KBIOGR_000231
KBIO3_000461
KBIOSS_000231
KBIO3_000462
KBIO2_005367
KBIO2_000231
LOPAC0_000472
NCGC00024605-05
NCGC00024605-04
CHEBI:107647
HMS1989L13
NCGC00024605-11
NCGC00024605-12
(-)-u-50488
CHEMBL58033
(-)-u-50488h
HMS1361L13
HMS1791L13
2-(3,4-dichlorophenyl)-n-methyl-n-[(2s)-2-(pyrrolidin-1-yl)cyclohexyl]acetamide
bdbm50000780
2-(3,4-dichloro-phenyl)-n-methyl-n-(2-pyrrolidin-1-yl-cyclohexyl)-acetamide
2-(3,4-dichlorophenyl)-n-methyl-n-[(1s,2s)-2-pyrrolidin-1-ylcyclohexyl]acetamide
NCGC00024605-10
CCG-204564
67198-19-0
(+/-) trans-u-50488 methanesulfonate
SCHEMBL10804846
trans-(-)-3,4-dichloro-n-methyl-n-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride
HMS3402L13
2-(3,4-dichlorophenyl)-n-methyl-n-[(1s,2s)-2-(1-pyrrolidinyl)cyclohexyl]acetamide
Q27185970
DTXSID10600858
(-)-u 50488
2-(3,4-dichlorophenyl)-n-methyl-n-((1s,2s)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide
(1s-trans)-3,4-dichloro-n-methyl-n-[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamide
BRD-K53532120-003-11-1
BRD-K53532120-003-03-8
SDCCGSBI-0050457.P004
NCGC00024605-17
NCGC00024605-18
u-50488-(-)
[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 (44)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.22390.100020.879379.4328AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency56.23410.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency24.56100.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.23660.001318.074339.8107AID926; AID938
regulator of G-protein signaling 4Homo sapiens (human)Potency0.91930.531815.435837.6858AID504845
67.9K proteinVaccinia virusPotency22.38720.00018.4406100.0000AID720580
arylsulfatase AHomo sapiens (human)Potency6.74561.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency17.65890.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.67850.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency15.84890.316212.443531.6228AID902
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.83440.00255.840031.6228AID899
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency70.79460.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency28.18380.006026.168889.1251AID488953
ras-related protein Rab-9AHomo sapiens (human)Potency58.04790.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency20.40540.00378.618923.2809AID2667; AID2668
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.96620.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.84890.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.84890.00638.235039.8107AID881
D(1A) dopamine receptorSus scrofa (pig)Potency14.68920.00378.108123.2809AID2667
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency6.26971.000010.475628.1838AID1457
GABA theta subunitRattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency17.90080.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.96621.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency45.15810.060110.745337.9330AID485368
[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)
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki5.00000.00000.60689.2330AID1781406
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki1.39700.00000.38458.6000AID1781405
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki0.00040.00000.18683.9500AID1191372
Kappa-type opioid receptorHomo sapiens (human)Ki0.17310.00000.362410.0000AID1255650; AID1781407
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Kappa-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.01700.00080.80564.8860AID1506426
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.03130.00000.22448.9900AID1781413; AID259400; AID592433
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Kappa-type opioid receptorHomo sapiens (human)ED500.02700.00071.45698.9400AID749676
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (57)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo 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 (15)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo 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 (25)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneKappa-type opioid receptorMus musculus (house mouse)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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 (58)

Assay IDTitleYearJournalArticle
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.
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.
AID149286Compound was evaluated for binding affinity towards kappa opioid receptor using [3H](-)-U-69,593 in guinea pig ileum1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID1781406Displacement of [3H]DPDPE from rat delta opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1781407Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID157446Compound was evaluated for binding affinity towards Phencyclidine receptor using [3H]TCP in guinea pig ileum; No inhibition at 10000 nM1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID1781417Antinociceptive activity in ip dosed Kunming mouse by hot plate test2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1255661Intrinsic activity at kappa opioid receptor in human HEK293 cells at 1 uM after 30 mins by [35S]GTPgammaS binding assay relative to U-695932015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID232473Selectivity ratio for affinities determined by using [3H]BREM and [3H]-(+)-3-PPP in guinea pig ileum1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID1781418Antinociceptive activity in ip dosed Kunming mouse assessed as reduction in acetic acid induced writhing signs measured after 15 mins by abdominal constriction test2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID259399Functional activity at human kappa opioid receptor expressed CHO cells by [35S]GTPgammaS binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID1506425Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy relative to DAMGO2017MedChemComm, Jan-01, Volume: 8, Issue:1
Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
AID1781414Agonist activity at human kappa opioid receptor expressed in CHO cell membrane at 1 uM incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1781409Selectivity ratio of Ki for displacement of [3H]DPDPE from rat delta opioid receptor expressed in CHO cell membrane to Ki for displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID259400Activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID1506427Agonist activity at mouse KOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy relative to U50488H2017MedChemComm, Jan-01, Volume: 8, Issue:1
Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
AID1781413Agonist activity at human kappa opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1255653Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1191372Displacement of [3H]U69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins2015European journal of medicinal chemistry, Jan-27, Volume: 90Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID1781424Induction of conditioned place aversion in mouse at 5 mg/kg, ip treated for 15 mins in the afternoon session of preconditioning phase by placing in preferred side for 30 mins followed by test phase after 24 hrs2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID749675Agonist activity at human recombinant kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding at 500 nM after 3 hrs by liquid scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
AID1506426Agonist activity at mouse KOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy2017MedChemComm, Jan-01, Volume: 8, Issue:1
Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
AID1191374Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in HEK cells after 60 mins2015European journal of medicinal chemistry, Jan-27, Volume: 90Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID595992Antinociceptive activity in Sprague-Dawley rat assessed as mean AUC of thermal-stimulus induced tail flick latency for 60 mins at 5 mg/kg, sc2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
AID592373Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting relative to control2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID1781408Selectivity ratio of Ki for displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cell membrane to Ki for displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1255660Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID203996Compound was evaluated for binding affinity towards sigma opioid receptor using [3H](+)-3-PPP in guinea pig ileum1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID1506424Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy2017MedChemComm, Jan-01, Volume: 8, Issue:1
Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
AID1781405Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method2021Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
Discovery of an
AID1191373Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in HEK cells after 60 mins2015European journal of medicinal chemistry, Jan-27, Volume: 90Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID749676Agonist activity at human recombinant kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
AID1255651Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1255650Binding affinity to kappa opioid receptor (unknown origin)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID592433Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID149287Compound was evaluated for binding affinity towards kappa opioid receptor using [3H]-BREM in guinea pig ileum1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID65265Compound was evaluated for binding affinity towards Dopamine receptor D2 using [3H]SULP in rat; No inhibition at 10000 nM1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
AID1255652Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (4.55)18.7374
1990's0 (0.00)18.2507
2000's2 (9.09)29.6817
2010's13 (59.09)24.3611
2020's6 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]