Page last updated: 2024-12-10

sr 144528

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

Description

SR 144528: a CB2 cannabinoid receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

SR 144528 : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-1H-pyrazole-3-carboxylic acid with the amino group of (1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-amine. A potent and selective cannabinoid receptor type 2 (CB2 receptor) inverse agonist (Ki = 0.6 nM). [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]

Cross-References

ID SourceID
PubMed CID3081355
CHEMBL ID381791
CHEBI ID146245
SCHEMBL ID8137029
MeSH IDM0286770

Synonyms (34)

Synonym
gtpl751
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-[(1s,4r,6s)-1,5,5-trimethyl-6-bicyclo[2.2.1]heptanyl]pyrazole-3-carboxamide
5-(4-chloro-3-methylphenyl)-1-((4-methylphenyl)methyl)-n-(1,3,3-trimethylbicyclo(2.2.1)hept-2-yl)-1h-pyrazole-3-carboxamide (1s-endo)-
1h-pyrazole-3-carboxamide, 5-(4-chloro-3-methylphenyl)-1-((4-methylphenyl)methyl)-n-(1,3,3-trimethylbicyclo(2.2.1)hept-2-yl)-, (1s-endo)-
sr 144528
sr-144528
sr144528
192703-06-3
5-(4-chloro-3-methyl-phenyl)-1-(4-methyl-benzyl)-1h-pyrazole-3-carboxylic acid ((1s,2s,4r)-1,3,3-trimethyl-bicyclo[2.2.1]hept-2-yl)-amide
bdbm50200170
5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-n-((1s,2s,4r)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl)-1h-pyrazole-3-carboxamide
CHEMBL381791 ,
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-[(1r,3s,4s)-2,2,4-trimethyl-3-bicyclo[2.2.1]heptanyl]pyrazole-3-carboxamide
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-[(1s,2s,4r)-1,3,3-trimethyl-2-bicyclo[2.2.1]heptanyl]pyrazole-3-carboxamide
5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-n-[(1s,2s,4r)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl]-1h-pyrazole-3-carboxamide
CHEBI:146245
sr144,528
SCHEMBL8137029
AKOS027323793
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-[(1s,2s,4r)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1h-pyrazole-3-carboxamide
J-012462
NCGC00386662-01
sr144528, >=98% (hplc)
EX-A7261
DTXSID50940947
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-(1,3,3-trimethyl-2-bicyclo[2.2.1]heptanyl)pyrazole-3-carboxamide
5-(4-chloro-3-methylphenyl)-1-((4-methylphenyl)methyl)-n-((1s,2s,4r)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl)-1h-pyrazole-3-carboxamide
CS-0006891
HY-13439
Q7392759
1h-pyrazole-3-carboxamide, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-n-[(1s,2s,4r)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-
MS-28830
cid 3081355
E98745

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

Bioavailability

ExcerptReferenceRelevance
" Clinical trials are now required, but are hindered by a paucity of cannabinoids of suitable bioavailability and therapeutic ratio."( Cannabinoids and pain.
Rice, AS, 2001
)
0.31
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" JTE-907 dosed orally inhibited carrageenin-induced mouse paw edema dose dependently."( In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.
Inaba, T; Iwamura, H; Kaya, T; Suzuki, H; Ueda, Y, 2001
)
0.31
" A leftward shift in the dose-response curve was observed following WIN55,212-2 relative to morphine treatment."( Activation of cannabinoid CB1 and CB2 receptors suppresses neuropathic nociception evoked by the chemotherapeutic agent vincristine in rats.
Hohmann, AG; Makriyannis, A; Rahn, EJ, 2007
)
0.34
" The effects of cumulative doses of abn-cbd (10(-9)-10(-5) M) on oxytocin-induced myometrial contractions alone, and on those following pre-incubation with SR 144528, AM 251, methylene blue, and iberiotoxin were measured, and dose-response curves were constructed."( Effects of abnormal cannabidiol on oxytocin-induced myometrial contractility.
Dennedy, MC; Houlihan, DD; Morrison, JJ, 2010
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
CB2 receptor antagonistAn antagonist that binds to and deactivates type 2 cannabinoid receptors.
EC 2.3.1.26 (sterol O-acyltransferase) inhibitorAn EC 2.3.1.* (acyltransferase transferring other than amino-acyl group) inhibitor that interferes with the action of acyl-CoA:cholesterol acyltransferase (EC 2.3.1.26).
[role 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]

Drug Classes (4)

ClassDescription
pyrazoles
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
bridged compoundA polycyclic compound in which two rings have two or more atoms in common.
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.89990.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency2.68370.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency2.68370.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
[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)IC50 (µMol)271.34720.00010.275310.0000AID1468646; AID1567164
Cannabinoid receptor 1Homo sapiens (human)Ki9.87120.00010.50779.6000AID1244366; AID1327379; AID1404263; AID1404264; AID1468646; AID1468648; AID1530506; AID1558585; AID1567165; AID1569940; AID1658162; AID660461
Cannabinoid receptor 2 Homo sapiens (human)IC50 (µMol)2.00900.00081.58409.8000AID1404267; AID1431665; AID1468641; AID1567166
Cannabinoid receptor 2 Homo sapiens (human)Ki0.12960.00000.415610.0000AID1244365; AID1244367; AID1327380; AID1404260; AID1404262; AID1468641; AID1468673; AID1530507; AID1558584; AID1567167; AID1569941; AID1658163; AID660462; AID768751; AID768753
[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)
Cannabinoid receptor 2 Homo sapiens (human)EC50 (µMol)5.85780.00030.15173.2800AID1569943; AID1569944; AID1658166; AID1719542; AID768748
Cannabinoid receptor 2Rattus norvegicus (Norway rat)EC50 (µMol)0.02330.00030.06660.3150AID768748
[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)Kieq2.82000.01200.01200.0120AID1286434
Cannabinoid receptor 2 Homo sapiens (human)Kieq0.00540.00380.26640.7900AID1286435
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (83)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo 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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (82)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1658164Selectivity index, ratio of Ki for recombinant human CB1R expressed in HEK293 cell membranes to Ki for recombinant human CB2R expressed in HEK293 cell membranes
AID1404270Inverse agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as increase in forskolin-stimulated cAMP level by BRET assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1193638Agonist activity at human cannabinoid CB2 receptor introduced into CHO cells assessed as [35S]GTPgammaS binding at 1 microM relative to control2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Loratadine analogues as MAGL inhibitors.
AID1327381Selectivity index, ratio of Ki for human CB1 receptor expressed in HEK293 cell membranes to Ki for human CB2 receptor expressed in HEK293 cell membranes2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID1567168Selectivity index, ratio of Ki for displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes to Ki for displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1404265Selectivity ratio of Ki for N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes to Ki for N-terminal HA-tagged human CB1 receptor expressed in HEK293 cell membrane2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1404264Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB1 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1719540Inverse agonist activity at cannabinoid CB1 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay2021Bioorganic & medicinal chemistry, 03-01, Volume: 33Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
AID1404280Effect on forskolin-stimulated cAMP level in HEK293 cells at 10 uM by BRET assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1286435Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solu
AID1567167Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins by Cheng-Prusoff equation analysis2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1404261Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB1 receptor expressed in HEK293 cell membranes at 10 uM after 1 hr by microbeta scintillation counting method relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1567165Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins by Cheng-Prusoff equation analysis2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1558572Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by spectrophotometry based Ellman's method2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.
AID660474Down-regulation of CB2 receptor protein level in human DU145 cells at 0.3 uM after 24 hrs by immunoblot analysis2012European journal of medicinal chemistry, Jun, Volume: 52Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
AID1468630Inhibition of human BChE using BTC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method
AID1658162Displacement of [3H]-CP-55,940 from recombinant human CB1R expressed in HEK293 cell membranes
AID1567166Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1404267Inverse agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as increase in forskolin-stimulated cAMP level by BRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1569943Agonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as increase of beta-arrestin recruitment by Tango assay
AID660473Antiproliferative activity against myelin basic protein-activated human lymphocytes at 0.3 uM2012European journal of medicinal chemistry, Jun, Volume: 52Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
AID1569958Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes at 10 uM incubated for 90 mins relative to control
AID1530509Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes at 10 uM measured after 90 mins relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
AID1530507Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes measured after 90 mins2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
AID1244367Displacement of [3H]-CP55940 from human CB2 receptor transfected in CHO cell membranes by liquid scintillation counting analysis2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
AID1327380Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID1404263Displacement of [3H]CP55,940 from human CB1 receptor2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID768753Binding affinity to human CB2 receptor expressed in CHO cells2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carbox
AID1431665Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay
AID1569941Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
AID1404273Activity at N-terminal HA-tagged human CB1 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as effect on forskolin-stimulated cAMP level by BRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1286436Selectivity index, ratio of Ki for recombinant human CB1 receptor to Ki for recombinant human CB2 receptor2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solu
AID1327379Displacement of [3H]-CP-55940 from human CB1 receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID1327386Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293 cell membranes at 1 to 10 uM after 90 mins relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID1404260Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1530506Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes measured after 90 mins2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
AID768748Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carbox
AID1569942Selectivity index, ratio of Ki for recombinant human CB1R expressed in HEK293 cell membranes to Ki for recombinant human CB2R expressed in HEK293 cell membranes
AID1468646Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method
AID768751Displacement of [3H]CP-55,940 from human CB2 receptor after 1 hr by competitive binding assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carbox
AID1404259Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes at 10 uM after 1 hr by microbeta scintillation counting method relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1569944Antagonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measure
AID1658163Displacement of [3H]-CP-55,940 from recombinant human CB2R expressed in HEK293 cell membranes
AID1327382Agonist activity at human CB2 receptor expressed in CHO-K1 cells assessed as reduction in NKH-477-induced intracellular cAMP levels after 30 mins in presence of NKH-477 by luminescence assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID660472Antiproliferative activity against human DU145 cells at 0.3 uM after 24 hrs by SRB assay in presence of CB2 receptor antagonist SR1445282012European journal of medicinal chemistry, Jun, Volume: 52Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
AID768750Selectivity ratio of Ki for rat brain CB2 receptor to Ki for rat spleen CB2 receptor2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carbox
AID1558584Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in human HEK cells by radioligand binding assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.
AID1244365Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
AID1244362Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
AID1286434Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solu
AID1468673Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 90 mins
AID1719542Inverse agonist activity at cannabinoid CB2 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay2021Bioorganic & medicinal chemistry, 03-01, Volume: 33Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
AID1404275Activity at N-terminal HA-tagged human CB1 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as effect on forskolin-stimulated cAMP level by BRET assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1468641Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method
AID1569940Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
AID1658166Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay
AID1558570Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by spectrophotometry based Ellman's method2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.
AID660461Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in human HEK293 cell membrane after 90 mins2012European journal of medicinal chemistry, Jun, Volume: 52Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
AID1468648Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 90 mins
AID1468635Inhibition of human erythrocyte AChE using ATC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method
AID1244366Displacement of [3H]-CP55940 from human CB1 receptor transfected in CHO cell membranes by liquid scintillation counting analysis2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
AID1404281Effect on forskolin-stimulated cAMP level in HEK293 cells at 1 uM by BRET assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1404262Displacement of [3H]CP55,940 from human CB2 receptor2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID768752Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carbox
AID1244361Antagonist/inverse agonist activity at CB2 receptor in mouse BV-2 cells assessed as inhibition of WIN55,212-2-mediated attenuation of LPS-induced PGE2 release at 10 uM after 16 hrs by ELISA immunoassay2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
AID1530508Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes at 10 uM measured after 90 mins relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
AID1569959Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes at 10 uM incubated for 90 mins relative to control
AID1530510Selectivity index, ratio of Ki for displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes to Ki for displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
AID1567164Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID660462Displacement of [3H]CP55940 from recombinant human CB2 receptor expressed in human HEK293 cell membrane after 90 mins2012European journal of medicinal chemistry, Jun, Volume: 52Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
AID1558585Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.
AID1719543Inverse agonist activity at cannabinoid CB2 receptor in human U2OS cells assessed as emission ratio using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay2021Bioorganic & medicinal chemistry, 03-01, Volume: 33Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
AID1327385Displacement of [3H]-CP-55940 from human CB1 receptor expressed in HEK293 cell membranes at 1 to 10 uM after 90 mins relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
AID1719541Inverse agonist activity at cannabinoid CB1 receptor in human U2OS cells assessed as emission ratio using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay2021Bioorganic & medicinal chemistry, 03-01, Volume: 33Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
AID1404277Inverse agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as increase in forskolin-stimulated cAMP level at 10 uM by BRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
AID1346728Human CB2 receptor (Cannabinoid receptors)1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630.
AID1346728Human CB2 receptor (Cannabinoid receptors)1998The Journal of pharmacology and experimental therapeutics, Feb, Volume: 284, Issue:2
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (257)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (5.45)18.2507
2000's150 (58.37)29.6817
2010's81 (31.52)24.3611
2020's12 (4.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.10

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.10 (24.57)
Research Supply Index5.57 (2.92)
Research Growth Index5.00 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (1.15%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other258 (98.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]