Page last updated: 2024-11-07

l 687384

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Description

L 687384: a high-affinity sigma receptor ligand [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID125328
CHEMBL ID303336
SCHEMBL ID467191
MeSH IDM0239563

Synonyms (34)

Synonym
bdbm50035097
1''-benzylspiro[1,2,3,4-tetrahydronaphthalene-1,4''-(hexahydropyridine)](l-687,384)
1''''-benzylspiro[1,2,3,4-tetrahydronaphthalene-1,4''''-(hexahydropyridine)]
1''''-benzyl-3,4-dihydro-2h-spiro[naphthalene-1,4''''-piperidine]; hcl
1''''-benzyl-3,4-dihydro-2h-spiro[naphthalene-1,4''''-piperidine](l-687,384)
lopac-l-8539
NCGC00015616-01
LOPAC0_000719
NCGC00162229-01
NCGC00015616-03
l 687384
l-687384
CHEMBL303336 ,
1'-benzylspiro[2,3-dihydro-1h-naphthalene-4,4'-piperidine]
95417-67-7
CCG-204804
AKOS016011471
NCGC00015616-02
l-687,384
3,4-dihydro-1'-(phenylmethyl)spiro(naphthalene-1(2h),4'-piperidine)
nve9k68qa3 ,
spiro(naphthalene-1(2h),4'-piperidine), 3,4-dihydro-1'-(phenylmethyl)-
1-benzyl-spiro(1,2,3,4-tetrahydronaphthalene-1,4-piperidine)
unii-nve9k68qa3
1'-benzyl-3,4-dihydro-2h-spiro[naphthalene-1,4'-piperidine]
MLDCBJPLHBPJET-UHFFFAOYSA-N
SCHEMBL467191
3,4-dihydro-1'-(phenylmethyl)spiro[naphthalene-1(2h),4'-piperidine]
DTXSID30241828
1'-benzyl-3,4-dihydro-2h-spiro(naphthalene-1,4'-piperidine)
Q6456075
spiro[naphthalene-1(2h),4'-piperidine], 3,4-dihydro-1'-(phenylmethyl)-
SDCCGSBI-0050697.P002
NCGC00015616-05

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" This potentiation is dose-dependent at doses between 1 and 1000 micrograms/kg, IV but bell-shaped dose-response curves are obtained."( Effects of low and high doses of selective sigma ligands: further evidence suggesting the existence of different subtypes of sigma receptors.
Bergeron, R; Debonnel, G, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.00530.100020.879379.4328AID488773; AID588453
ATAD5 protein, partialHomo sapiens (human)Potency14.33360.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency3.16230.00308.794948.0869AID1347053
NFKB1 protein, partialHomo sapiens (human)Potency0.35480.02827.055915.8489AID895; AID928
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.11890.001318.074339.8107AID926; AID938
polyproteinZika virusPotency3.16230.00308.794948.0869AID1347053
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency21.19230.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.25120.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency19.95260.316212.443531.6228AID902
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.00000.00255.840031.6228AID899
D(1A) dopamine receptorHomo sapiens (human)Potency4.10920.02245.944922.3872AID488982
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID995
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency23.28090.00378.618923.2809AID2668
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency25.11890.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.29470.00106.000935.4813AID943; AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
[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)
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)7.10000.00011.753610.0000AID5491
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)7.10000.00040.908610.0000AID5491
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00021.874210.0000AID37007
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)50.50000.00031.38338.4000AID37007; AID4136
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00021.270410.0000AID37007
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00051.48357.8000AID37007
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00311.73607.8000AID37007
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00501.79627.8000AID37007
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00001.819410.0000AID37007
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)3.70000.00010.54948.4000AID64613
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki0.04400.00241.10509.3000AID1845724
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.00200.00000.338510.0000AID1845723
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.00030.00030.70285.3660AID204763
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00030.00030.55704.2000AID204762; AID204763
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo 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)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo 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)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus 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)
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)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (40)

Assay IDTitleYearJournalArticle
AID204462Binding affinity for sigma receptor of guinea pig whole brain using [3H]-SKF- 100047 radioligand1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID1845725Selectivity ratio of Ki for rat liver Sigma2 receptor to Ki for Guinea pig brain Sigma1 receptor2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Spirocyclic Scaffolds in Medicinal Chemistry.
AID225350Antimescaline activity in the mouse (administered po)1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID1393295Displacement of [3H]-DTG from sigma-2 receptor in rat liver membranes after 180 mins by scintillation counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
AID225346Ability to block the aggressive behavior caused by prolonged isolation in mouse (administered po)1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID204762Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID1845723Binding affinity to Guinea pig brain Sigma1 receptor assessed as inhibition constant2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Spirocyclic Scaffolds in Medicinal Chemistry.
AID204772Binding affinity towards sigma receptor binding site 2 using [3H]DTG of whole rat brain homogenates except cerebellum1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID204771Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID64613Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID176971In vivo antagonism of compound determined by the ability to inhibit 5-HTP-induced head twitch in rat (administered po)1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID62740Binding affinity for dopamine D2 receptor using [3H]spiperone in guinea pig striatum1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID204764Ratio of the binding affinities against Sigma receptor type 1 and Sigma receptor type 21995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID5011Binding affinity for serotonin 5-hydroxytryptamine 2 receptor using [3H]ketanserin in guinea pig frontal cortex1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
Piperidinyltetralin sigma ligands.
AID4136Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. 1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID204763Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID1845724Binding affinity to rat liver Sigma2 receptor assessed as inhibition constant2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Spirocyclic Scaffolds in Medicinal Chemistry.
AID1393294Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
AID230925Binding affinities for sigma-1 and sigma 2 receptors, ratio of IC501995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID37007Binding affinity towards Alpha-1 adrenergic receptor binding site using [3H]prazosin.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID5491Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. 1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
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.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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 (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (26.32)18.2507
2000's2 (10.53)29.6817
2010's6 (31.58)24.3611
2020's6 (31.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.88

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 Index11.88 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.87 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (10.53%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (89.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]