Page last updated: 2024-12-10

jhw 015

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

Cross-References

ID SourceID
PubMed CID4273754
CHEMBL ID306764
CHEBI ID92318
SCHEMBL ID497044
MeSH IDM0355707

Synonyms (43)

Synonym
MLS002153392
smr001230773
HMS3267P11
BRD-K17796732-001-02-0
jwh-015, >=98% (hplc), powder
tocris-1341
NCGC00025117-01 ,
chembl306764 ,
bdbm21282
2-methyl-3-(naphthalen-1-ylcarbonyl)-1-propyl-1h-indole
jwh-015
jwh015
jhw-015
(2-methyl-1-propyl-1h-indol-3-yl)-1-naphthalenylmethanone
jwh 015
jhw 015
1-propyl-2-methyl-3-(1-naphthoyl)indole
(2-methyl-1-propyl-1h-indol-3-yl)-1-naphthalenyl-methanone
methanone, (2-methyl-1-propyl-1h-indol-3-yl)-1-naphthalenyl-
(2-methyl-1-propylindol-3-yl)-naphthalen-1-ylmethanone
w4fl204t10 ,
155471-08-2
unii-w4fl204t10
HMS2236B06
AKOS015909302
gtpl5558
HMS3373A11
CCG-208734
j771.996e ,
SCHEMBL497044
jwh-015 (1-propyl-2-methyl-3-(1-napthoyl)indole)
LJSBBBWQTLXQEN-UHFFFAOYSA-N
HMS3650K06
DTXSID60165902
SR-01000597570-1
sr-01000597570
CHEBI:92318
jwh-015 ((2-methyl-1-propylindol-3-yl)(naphthalen-1-yl)methanone) 1.0 mg/ml in acetonitrile
jwh-015; (2-methyl-1-propylindol-3-yl)(naphthalen-1-yl)methanone
jwh-015 ((2-methyl-1-propylindol-3-yl)(naphthalen-1-yl)methanone) 0.1 mg/ml in acetonitrile
jwh-015 ((2-methyl-1-propylindol-3-yl)(naphthalen-1-yl)methanone)
Q6109176
SR-01000597570-3

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" 2 Delta(9)-and Delta(8)-tetrahydrocannabinol (THC) were toxic when added directly to SH-SY5Y neuroblastoma cells."( Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor.
Bissonnette, CJ; Klegeris, A; McGeer, PL, 2003
)
0.32
" In this study we compared the effects of CB1 and CB2 receptor-selective ligands, the endocannabinoid anandamide and the phytocannabinoid cannabidiol, against oxidative stress and the toxic hallmark Alzheimer's protein, β-amyloid (Aβ) in neuronal cell lines."( Contrasting protective effects of cannabinoids against oxidative stress and amyloid-β evoked neurotoxicity in vitro.
Harvey, BS; Mååg, JL; Musgrave, IF; Ohlsson, KS; Smid, SD, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indolecarboxamide
[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 (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency37.93300.007215.758889.3584AID588342
glp-1 receptor, partialHomo sapiens (human)Potency14.12540.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency11.57740.004110.890331.5287AID504466
USP1 protein, partialHomo sapiens (human)Potency19.95260.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency21.01790.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency42.23950.180013.557439.8107AID1460; AID1468
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency12.58930.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.58930.001318.074339.8107AID926; AID938
glucocerebrosidaseHomo sapiens (human)Potency28.18380.01268.156944.6684AID2101
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.00000.00255.840031.6228AID899
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency11.22020.001815.663839.8107AID894
mitogen-activated protein kinase 1Homo sapiens (human)Potency19.95260.039816.784239.8107AID995
gemininHomo sapiens (human)Potency25.92900.004611.374133.4983AID624296
lethal factor (plasmid)Bacillus anthracis str. A2012Potency2.51190.020010.786931.6228AID912
TAR DNA-binding protein 43Homo sapiens (human)Potency0.31621.778316.208135.4813AID652104
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency7.94333.981146.7448112.2020AID720708
[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)
Cannabinoid receptor 1Homo sapiens (human)Ki0.80010.00010.50779.6000AID1127518; AID1798067; AID324969; AID444910; AID569312; AID769550
Cannabinoid receptor 2 Homo sapiens (human)Ki0.13370.00000.415610.0000AID1127517; AID1798067; AID238798; AID324968; AID419195; AID444909; AID569313; AID769551
Bile acid receptorHomo sapiens (human)IC50 (µMol)3.22000.01834.560310.0000AID755454
[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)
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)2.64000.00203.519610.0000AID755445
Cannabinoid receptor 2 Homo sapiens (human)EC50 (µMol)0.63400.00030.15173.2800AID324971; AID444912
Cannabinoid receptor 2Mus musculus (house mouse)EC50 (µMol)0.09500.00730.15460.7040AID1573480; AID1573482
[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)
Cannabinoid receptor 1Homo sapiens (human)Log Ki0.00260.00030.00190.0036AID49325
Cannabinoid receptor 2 Homo sapiens (human)Log Ki0.00110.00050.00200.0035AID49851
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (119)

Processvia Protein(s)Taxonomy
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of acute inflammatory response to antigenic stimulusCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
spermatogenesisCannabinoid receptor 1Homo sapiens (human)
axonal fasciculationCannabinoid receptor 1Homo sapiens (human)
response to nutrientCannabinoid receptor 1Homo sapiens (human)
memoryCannabinoid receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentCannabinoid receptor 1Homo sapiens (human)
negative regulation of serotonin secretionCannabinoid receptor 1Homo sapiens (human)
positive regulation of fever generationCannabinoid receptor 1Homo sapiens (human)
negative regulation of fatty acid beta-oxidationCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, GABAergicCannabinoid receptor 1Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 1Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 1Homo sapiens (human)
negative regulation of dopamine secretionCannabinoid receptor 1Homo sapiens (human)
response to nicotineCannabinoid receptor 1Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 1Homo sapiens (human)
response to cocaineCannabinoid receptor 1Homo sapiens (human)
glucose homeostasisCannabinoid receptor 1Homo sapiens (human)
positive regulation of apoptotic processCannabinoid receptor 1Homo sapiens (human)
response to ethanolCannabinoid receptor 1Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 1Homo sapiens (human)
negative regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
positive regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
regulation of insulin secretionCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicCannabinoid receptor 1Homo sapiens (human)
maternal process involved in female pregnancyCannabinoid receptor 1Homo sapiens (human)
regulation of feeding behaviorCannabinoid receptor 1Homo sapiens (human)
regulation of penile erectionCannabinoid receptor 1Homo sapiens (human)
retrograde trans-synaptic signaling by endocannabinoidCannabinoid receptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationCannabinoid receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 1Homo sapiens (human)
response to amphetamineCannabinoid receptor 2 Homo sapiens (human)
inflammatory responseCannabinoid receptor 2 Homo sapiens (human)
immune responseCannabinoid receptor 2 Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 2 Homo sapiens (human)
leukocyte chemotaxisCannabinoid receptor 2 Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicCannabinoid receptor 2 Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 2 Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 2 Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 2 Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 2 Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 2 Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 2 Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
negative regulation of very-low-density lipoprotein particle remodelingBile acid receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionBile acid receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
nitrogen catabolite activation of transcription from RNA polymerase II promoterBile acid receptorHomo sapiens (human)
intracellular glucose homeostasisBile acid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
inflammatory responseBile acid receptorHomo sapiens (human)
cell-cell junction assemblyBile acid receptorHomo sapiens (human)
Notch signaling pathwayBile acid receptorHomo sapiens (human)
bile acid metabolic processBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathwayBile acid receptorHomo sapiens (human)
regulation of low-density lipoprotein particle clearanceBile acid receptorHomo sapiens (human)
intracellular receptor signaling pathwayBile acid receptorHomo sapiens (human)
negative regulation of type II interferon productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-1 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-2 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-6 productionBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionBile acid receptorHomo sapiens (human)
positive regulation of interleukin-17 productionBile acid receptorHomo sapiens (human)
toll-like receptor 9 signaling pathwayBile acid receptorHomo sapiens (human)
regulation of urea metabolic processBile acid receptorHomo sapiens (human)
intracellular triglyceride homeostasisBile acid receptorHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
bile acid signaling pathwayBile acid receptorHomo sapiens (human)
intracellular bile acid receptor signaling pathwayBile acid receptorHomo sapiens (human)
cholesterol homeostasisBile acid receptorHomo sapiens (human)
defense response to bacteriumBile acid receptorHomo sapiens (human)
negative regulation of apoptotic processBile acid receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionBile acid receptorHomo sapiens (human)
innate immune responseBile acid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayBile acid receptorHomo sapiens (human)
fatty acid homeostasisBile acid receptorHomo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
regulation of bile acid biosynthetic processBile acid receptorHomo sapiens (human)
cellular response to lipopolysaccharideBile acid receptorHomo sapiens (human)
cellular response to fatty acidBile acid receptorHomo sapiens (human)
cellular response to organonitrogen compoundBile acid receptorHomo sapiens (human)
negative regulation of monocyte chemotactic protein-1 productionBile acid receptorHomo sapiens (human)
regulation of cholesterol metabolic processBile acid receptorHomo sapiens (human)
cellular response to bile acidBile acid receptorHomo sapiens (human)
positive regulation of adipose tissue developmentBile acid receptorHomo sapiens (human)
positive regulation of phosphatidic acid biosynthetic processBile acid receptorHomo sapiens (human)
positive regulation of glutamate metabolic processBile acid receptorHomo sapiens (human)
positive regulation of ammonia assimilation cycleBile acid receptorHomo sapiens (human)
cell differentiationBile acid receptorHomo sapiens (human)
negative regulation of inflammatory responseBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cannabinoid receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 1Homo sapiens (human)
identical protein bindingCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 2 Homo sapiens (human)
cannabinoid receptor activityCannabinoid receptor 2 Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
transcription coregulator bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activityBile acid receptorHomo sapiens (human)
nuclear receptor activityBile acid receptorHomo sapiens (human)
protein bindingBile acid receptorHomo sapiens (human)
zinc ion bindingBile acid receptorHomo sapiens (human)
nuclear receptor bindingBile acid receptorHomo sapiens (human)
bile acid bindingBile acid receptorHomo sapiens (human)
bile acid receptor activityBile acid receptorHomo sapiens (human)
sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
nuclear retinoid X receptor bindingBile acid receptorHomo sapiens (human)
chenodeoxycholic acid bindingBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
mitochondrial outer membraneCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
actin cytoskeletonCannabinoid receptor 1Homo sapiens (human)
growth coneCannabinoid receptor 1Homo sapiens (human)
presynaptic membraneCannabinoid receptor 1Homo sapiens (human)
membrane raftCannabinoid receptor 1Homo sapiens (human)
glutamatergic synapseCannabinoid receptor 1Homo sapiens (human)
GABA-ergic synapseCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
cytoplasmCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 2 Homo sapiens (human)
dendriteCannabinoid receptor 2 Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneCannabinoid receptor 2 Homo sapiens (human)
perikaryonCannabinoid receptor 2 Homo sapiens (human)
endoplasmic reticulumCannabinoid receptor 2 Homo sapiens (human)
plasma membraneCannabinoid receptor 2 Homo sapiens (human)
cytoplasmCannabinoid receptor 2 Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
nucleoplasmBile acid receptorHomo sapiens (human)
chromatinBile acid receptorHomo sapiens (human)
euchromatinBile acid receptorHomo sapiens (human)
receptor complexBile acid receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexBile acid receptorHomo sapiens (human)
nucleusBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
AID1127517Binding affinity to CB2 receptor (unknown origin)2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID324970Selectivity for human recombinant CB2 receptor over human recombinant CB1 receptor2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1573483Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay relative 2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID444911Selectivity ratio of Ki for human recombinant CB1 receptor to Ki for human recombinant CB2 receptor2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
AID755449Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation at 40 uM after 16 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID714694Locomotor activity in iv dosed Harlan ICR mouse from 5 to 15 mins by spontaneous locomotor activity test2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
AID49325Binding affinity towards cloned human Cannabinoid receptor 12000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.
AID324968Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID371692Cytotoxicity against human U87MG cells at 10 uM after 48 hrs by WST1 assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID324969Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID444913Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay relative to CP-559402010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
AID714949Induction of catalepsy in mouse by ring immobility test2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
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.
AID1573536Ratio of EC50 for C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment to EC50 for mouse CB2 receptor expressed in HEK293 cells as2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID375666Cytotoxicity against human U87MG cells after 48 hrs by WST1 assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
AID569314Selectivity ratio of Ki for human CB1 to Ki for human CB22011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.
AID375665Cytotoxicity against human Jurkat cells after 48 hrs by WST1 assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
AID1573480Inverse agonist activity at mouse CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 5 mins by fluorescence assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID714717Hypothermic activity in iv dosed Harlan ICR mouse assessed as change in rectal temperature at 30 mins2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
AID1127518Binding affinity to CB1 receptor (unknown origin)2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID419195Displacement of [3H]CP-55940 from human cloned CB2 receptor by filtration assay2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.
AID1573482Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID714689Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
AID755454Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID444910Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID755445Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
AID769550Binding affinity to CB1 receptor (unknown origin)2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Contributions of academic laboratories to the discovery and development of chemical biology tools.
AID769551Binding affinity to CB2 receptor (unknown origin)2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Contributions of academic laboratories to the discovery and development of chemical biology tools.
AID324971Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID419197Selectivity ratio of pKi for human cloned CB2 receptor to pKi for CB1 receptor in rat brain2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.
AID755455Antagonist activity at human GTS-tagged FXR at 15 uM after 20 mins by TR-FRET assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
AID569313Displacement of [3H]CP 55940 from human CB2 receptor in cell free system2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.
AID419196Selectivity ratio of pKi for CB1 receptor in rat brain to pKi for human cloned CB2 receptor2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.
AID243372Percentage ([35S]GTP-gamma-S binding was determined from basal towards human cannabinoid receptor 2 at 1 uM concentration using fluorescence assay2005Bioorganic & medicinal chemistry letters, Aug-15, Volume: 15, Issue:16
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
AID569312Displacement of [3H]CP 55940 from human CB1 receptor in cell free system2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.
AID324972Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR relative to CP-559402008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID49851Binding affinity towards cloned human cannabinoid receptor 22000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.
AID1573481Inverse agonist activity at mouse CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 5 mins by fluorescence assay relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID714707Antinociceptive activity in iv dosed Harlan ICR mouse assessed as latency to heat-induced tail flicking at 20 mins2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
AID444909Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
AID444912Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
AID769549Selectivity ratio of Ki for CB1 receptor (unknown origin) to Ki for CB2 receptor (unknown origin)2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Contributions of academic laboratories to the discovery and development of chemical biology tools.
AID238798In vitro inhibitory activity towards human cannabinoid receptors 2 using fluorescence assay2005Bioorganic & medicinal chemistry letters, Aug-15, Volume: 15, Issue:16
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
AID419194Displacement of [3H]CP-55940 from CB1 receptor in rat brain by filtration assay2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1798067Radioligand Binding Assay from Article 10.1021/jm7011613: \\Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.\\2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
AID1345070Human GPR55 (GPR18, GPR55 and GPR119)2007British journal of pharmacology, Dec, Volume: 152, Issue:7
The orphan receptor GPR55 is a novel cannabinoid receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (105)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (0.95)18.2507
2000's41 (39.05)29.6817
2010's60 (57.14)24.3611
2020's3 (2.86)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%
Reviews5 (4.72%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other101 (95.28%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]