Page last updated: 2024-11-12

1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea

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Description

1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11560249
CHEMBL ID3341861
SCHEMBL ID4924047
MeSH IDM0518612

Synonyms (30)

Synonym
SCHEMBL4924047
1-(4-chlorophenyl)-3-(3-(6-(pyrrolidin-1-yl)pyridin-2-yl)phenyl)urea
HDAYFSFWIPRJSO-UHFFFAOYSA-N
1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl]urea
AKOS025142088
1-(4-chloro-phenyl)-3-[3-(6-pyrrolidin-1-yl-pyridin-2-yl)-phenyl]-urea
psncbam-1
n-(4-chlorophenyl)-n'-[3-[6-(1-pyrrolidinyl)-2-pyridinyl]phenyl]urea
psncbam 1
877202-74-9
bdbm50023629
CHEMBL3341861 ,
1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl] urea
psncbam-1, >=98% (hplc)
NCGC00386583-02
1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea
psncbam1
BCP27729
psncbam 1;psncbam1
TQR1361
1-(4-chlorophenyl)-3-[3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl]urea
CS-0033043
n-(4-chlorophenyl)-n'-(3-(6-(1-pyrrolidinyl)-2-pyridinyl)phenyl)urea
urea, n-(4-chlorophenyl)-n'-(3-(6-(1-pyrrolidinyl)-2-pyridinyl)phenyl)-
P34SC5V6W2 ,
unii-p34sc5v6w2
CKB20274
HY-110179
DTXSID701046393
E98864

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.00810.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency6.74120.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[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)
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50 (µMol)2.10000.00020.59827.0000AID1366772
Cannabinoid receptor 1Homo sapiens (human)IC50 (µMol)0.29660.00010.275310.0000AID1161647; AID1366768; AID1458798; AID1458805; AID1532933; AID1532935; AID1616820; AID1616824; AID1616825; AID1616832; AID1616833; AID1776934; AID1776935; AID1776936
Cannabinoid receptor 2 Homo sapiens (human)IC50 (µMol)10.00000.00081.58409.8000AID1161649; AID1458800; AID1616819; AID1776939
Cannabinoid receptor 2 Homo sapiens (human)Ki10.00000.00000.415610.0000AID1366769
Cannabinoid receptor 1Mus musculus (house mouse)IC50 (µMol)0.28500.00300.92943.2000AID1616822; AID1616825
Monoglyceride lipaseHomo sapiens (human)IC50 (µMol)100.00000.00091.126810.0000AID1366773
[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 1Homo sapiens (human)EC50 (µMol)0.12790.00010.12752.2400AID1161652; AID1273373; AID1273375; AID1366765
[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)Kb0.05420.00070.38172.2000AID1426535; AID1616821
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (95)

Processvia Protein(s)Taxonomy
fatty acid catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
arachidonic acid metabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
positive regulation of vasoconstrictionFatty-acid amide hydrolase 1Homo sapiens (human)
monoacylglycerol catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
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)
lipid metabolic processMonoglyceride lipaseHomo sapiens (human)
fatty acid biosynthetic processMonoglyceride lipaseHomo sapiens (human)
inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of signal transductionMonoglyceride lipaseHomo sapiens (human)
arachidonic acid metabolic processMonoglyceride lipaseHomo sapiens (human)
triglyceride catabolic processMonoglyceride lipaseHomo sapiens (human)
acylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of sensory perception of painMonoglyceride lipaseHomo sapiens (human)
monoacylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of endocannabinoid signaling pathwayMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
phospholipid bindingFatty-acid amide hydrolase 1Homo sapiens (human)
fatty acid amide hydrolase activityFatty-acid amide hydrolase 1Homo sapiens (human)
identical protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
acylglycerol lipase activityFatty-acid amide hydrolase 1Homo sapiens (human)
amidase activityFatty-acid amide hydrolase 1Homo sapiens (human)
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)
lysophospholipase activityMonoglyceride lipaseHomo sapiens (human)
protein bindingMonoglyceride lipaseHomo sapiens (human)
protein homodimerization activityMonoglyceride lipaseHomo sapiens (human)
acylglycerol lipase activityMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneFatty-acid amide hydrolase 1Homo sapiens (human)
cytoskeletonFatty-acid amide hydrolase 1Homo sapiens (human)
organelle membraneFatty-acid amide hydrolase 1Homo sapiens (human)
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)
endoplasmic reticulum membraneMonoglyceride lipaseHomo sapiens (human)
cytosolMonoglyceride lipaseHomo sapiens (human)
plasma membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1458811Reduction in cocaine-induced reinstatement of cocaine seeking behavior in Sprague-Dawley rat at 30 mg/kg pretreated for 10 mins followed by cocaine treatment on day following last extinction session2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1776939Antagonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec for 90 secs 2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1458809Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1458810Clearance in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1776936Allosteric antagonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in HEK293 cells assessed as reduction in CP55940-stimulated inhibition of forskolin-induced cAMP accumulation measured for 20 mins by BRET assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1458803Allosteric modulation of CB1 receptor in CD-1 mouse cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding after 60 mins2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1616828Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as increase in specific binding of [3H]CP55,940 incubated for 90 mins by radioligand binding assay relative to control2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616819Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1426536Allosteric modulation at CB1 receptor (unknown origin) expressed in HEK293T cell membranes assessed as inhibition of CP55,940 induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
AID1426535Positive allosteric modulation of CB1 receptor (unknown origin) expressed in HEK293T cell membranes assessed as increase in [3H]CP55,940 binding by liquid scintillation counting method
AID1776940Agonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as stimulation of calcium mobilization measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay relative to Emax of CP559402021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1161647Antagonist activity at human CB1 receptor stably expressed in RD-HGA16 cells assessed as inhibition of CP55,940-induced calcium mobilization after 15 mins by FLIPR assay2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
AID1458804Allosteric modulation of CB1 receptor in rat cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1273373Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
AID1616825Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1458805Allosteric modulation of CB1 receptor in HEK293 cell membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1616821Displacement of [3H]CP55,940 from human CB1 receptor2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1458800Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calciu2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1366770Inhibition of FAAH in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels up to 10 uM preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1366774Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1616820Allosteric antagonist activity at human CB1 receptor by Ca2+ assay2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1776934Allosteric antagonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec f2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1616823Half life in rat liver microsomes2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1532934Agonist activity at CB1 receptor (unknown origin) relative to CP559402018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Allosteric CB
AID1776935Allosteric antagonist activity at human CB1 receptor expressed in HEK293 cell membrane assessed as inhibition of CP55940-stimulated [35S]GTPgammaS binding incubated for 60 mins by [35S]GTP-gammaS binding assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1616834Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding at 10 uM incubated for 60 mins by scintillation counting method2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1458799Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,9402017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1616838Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616833Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616841Apparent permeability from apical to basolateral side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616830Agonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,9402019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1161648Agonist activity at human CB1 receptor stably expressed in RD-HGA16 cells assessed as calcium mobilization at 10000 nM after 15 mins by FLIPR assay relative to CP55,9402014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
AID1616843Efflux ratio from basolateral to apical side over apical to basolateral side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616822Allosteric antagonist activity at mouse CB1 receptor by GTPgammaS assay2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1161652Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
AID1161649Antagonist activity at human CB2 receptor stably expressed in CHO-RD-HGA16 cells assessed as inhibition of CP55,940-induced calcium mobilization after 15 mins by FLIPR assay2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
AID1616842Apparent permeability from basolateral to apical side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616826Allosteric modulator activity at CB1 receptor in mouse cerebellar membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1366773Inhibition of MAGL in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1616824Allosteric modulator activity at human CB1 receptor expressed in CHO-RD-HGA16 cells co-expressing Galpha16 assessed as suppression of 100 nM CP55,940-induced calcium mobilization pre-incubated for 15 mins by Calcium 5 dye based FLIPR assay2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616837Ratio of IC50 for allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method IC50 for allosteric m2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1776937Agonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as stimulation of calcium mobilization measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay relative to Emax of CP559402021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1366772Inhibition of FAAH in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1616836Allosteric modulator activity at CB1 receptor in mouse cerebellar membranes assessed as suppression of 1 uM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1273375Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
AID1616840Kinetic solubility in phosphate buffer at 400 uM incubated for 2 hrs by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616832Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1532935Allosteric modulation of CB1 receptor (unknown origin) assessed as inhibition of CP55940-induced [35S]GTPgammaS binding2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Allosteric CB
AID1458806PAM antagonist activity at CB1 receptor in CD-1 mouse cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding after 60 mins2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1426538Positive allosteric modulation of CB1 receptor (unknown origin) expressed in HEK293T cell membrane assessed as ERK1/2 phosphorylation in presence of beta-arrestin1 siRNA at 10 uM incubated for 5 mins by Western blot method
AID1273376Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
AID1161653Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting relative to control2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
AID1776938Antagonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization at 10 uM preincubated for 15 mins followed by agonist addition and measured every 1 sec for2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
AID1366769Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO-K1 cell membranes after 1.5 hrs by liquid scintillation counting assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1458801Agonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,9402017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1532933Allosteric modulation of CB1 receptor (unknown origin) assessed as inhibition of calcium mobilization by FLIPR assay2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Allosteric CB
AID1366771Inhibition of MAGL in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels up to 10 uM preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1458798Allosteric modulation of human CB1 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calc2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
AID1366765Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cell membranes assessed as induction of [3H]CP55,940 binding after 1.5 hrs by liquid scintillation counting assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1616831Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization at 10 uM preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1366764Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cell membranes assessed as induction of [3H]CP55,940 binding at 0.001 to 100 uM after 1.5 hrs by liquid scintillation counting assay relative to control2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1273374Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay relative to2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
AID1366768Negative allosteric modulation of human CB1 receptor expressed in HEK293 cells assessed as inhibition of 33 nM CP55,940-induced SRE transcriptional activity after 5 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
AID1616839Clearance in rat liver microsomes in presence of NADPH incubated up to 45 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
AID1616829Agonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells co-expressing Galpha16 assessed as suppression stimulation of calcium mobilization incubated for 45 mins by Calcium 5 dye based FLIPR assay relative to CP55,9402019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (4.35)29.6817
2010's17 (73.91)24.3611
2020's5 (21.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.10

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

MetricThis Compound (vs All)
Research Demand Index13.10 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index6.27 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.35%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (95.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]