Page last updated: 2024-11-13

jzl195

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Description

JZL195: inhibits both ​fatty-acid amide hydrolase 1 and ​monoglyceride lipase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46232606
CHEMBL ID606201
SCHEMBL ID19744767
MeSH IDM000598641

Synonyms (40)

Synonym
CHEMBL606201 ,
bdbm50307083
4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate
jzl195
NCGC00346837-01
S6609
CS-3374
HY-15250
MLS006010728
smr004701690
1210004-12-8
jzl 195 ,
4-[(3-phenoxyphenyl)methyl]-1-piperazinecarboxylic acid 4-nitrophenyl ester
jzl-195
gtpl8606
(4-nitrophenyl) 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate
AKOS024458308
QNYRAEKLMNDRFY-UHFFFAOYSA-N
J-004424
EX-A635
4-nitrophenyl 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate
jzl195, >=98% (hplc)
NCGC00346837-02
jzl-195; jzl 195
BCP23894
Q6109295
mfcd18382122
FT-0700116
BS-14525
SCHEMBL19744767
nsc-763527
nsc763527
4-nitrophenyl 4-(3-phenoxybenzyl)-1-piperazinecarboxylate
DTXSID401029877
1-piperazinecarboxylic acid, 4-[(3-phenoxyphenyl)methyl]-, 4-nitrophenyl ester
4-nitrophenyl 4-[(3-phenoxyphenyl)methyl]-1-piperazinecarboxylate
tp6p2hkj54 ,
4-nitrophenyl 4-((3-phenoxyphenyl)methyl)-1-piperazinecarboxylate
unii-tp6p2hkj54
AC-36809

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

Dosage Studied

ExcerptRelevanceReference
"6 mg/kg) served as a discriminative stimulus in both genotypes, with similar THC dose-response curves between groups."( Phenotypic assessment of THC discriminative stimulus properties in fatty acid amide hydrolase knockout and wildtype mice.
Vann, RE; Walentiny, DM; Wiley, JL, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency13.13730.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency29.56590.001310.157742.8575AID1259253
GVesicular stomatitis virusPotency18.99910.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency2.68370.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency14.60270.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
[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)0.00770.00020.59827.0000AID1867628; AID1890731; AID1891959
Monoglyceride lipaseHomo sapiens (human)IC50 (µMol)0.07080.00091.126810.0000AID1655068; AID1890732; AID1891960
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (58)

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)
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 (25)

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)
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 (25)

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)
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 (63)

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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
AID1891960Inhibition of recombinant MAGL (unknown origin) expressed in COS7 cells assessed as blockade of substrate hydrolysis using AEA as substrate preincubated with compound for 30 mins followed by susbstrate addition2022Bioorganic & medicinal chemistry letters, 07-15, Volume: 68Design and synthesis of endocannabinoid enzyme inhibitors for ocular indications.
AID703152Inhibition of bacterial lipoprotein lipase at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID703155Inhibition of mouse DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 10000 nM by scintillation counting based radio-TLC assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID1890732Inhibition of human recombinant MAGL incubated for 5 mins followed by substrate addition by cayman fluorescence based multimode microplate reader assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
AID703150Inhibition of porcine pancreatic lipase type 2 at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID703158Inhibition of mouse DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 10 nM by scintillation counting based radio-TLC assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID703171Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 10 uM using JZL184 pretreated protein in detergent free solution by FRET assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID1867628Inhibition of human recombinant FAAH using AMC-AA as substrate preincubated with enzyme for 10 mins followed by substrate addition for 2 hrs by fluorometric analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
AID458310Toxicity in mouse assessed as death at 20 mg/kg, ip for 6 days2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID703157Inhibition of mouse DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 100 nM by scintillation counting based radio-TLC assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID458301Inhibition of MAGL in mouse brain membrane2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID458309In vivo inhibition of MAGL in mouse at 100 mg/kg, po2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID1655068Inhibition of human recombinant MAGL pre-incubated for 5 mins before MAGL substrate addition and further incubated for 10 mins2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
AID458304Inhibition of NTE in mouse brain membrane2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID1867627Inhibition of human BuChE by Ellman's spectrophotometric method2022European journal of medicinal chemistry, Jul-05, Volume: 237Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
AID1890731Inhibition of recombinant human FAAH incubated for 5 mins followed by substrate addition by cayman fluorescence based multimode microplate reader assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
AID458302Inhibition of ABHD6 in mouse brain membrane2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID458306In vivo inhibition of FAAH in mouse at 20 mg/kg, ip2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID458300Inhibition of FAAH in mouse brain membrane2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID703154Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 10 uM in detergent free solution by FRET assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID458307In vivo inhibition of FAAH in mouse at 100 mg/kg, po2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID703156Inhibition of mouse DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 1000 nM by scintillation counting based radio-TLC assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID1053375Inhibition of TAMRA-FP-labeled FAAH in mouse brain membrane at 10 uM after 1 hr by fluorescent gel scanning assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.
AID1891959Inhibition of recombinant FAAH (unknown origin) expressed in COS7 cells assessed as blockade of substrate hydrolysis using 2-AG as substrate preincubated with compound for 30 mins followed by substrate addition2022Bioorganic & medicinal chemistry letters, 07-15, Volume: 68Design and synthesis of endocannabinoid enzyme inhibitors for ocular indications.
AID1867626Inhibition of human AChE by Ellman's spectrophotometric method2022European journal of medicinal chemistry, Jul-05, Volume: 237Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
AID703169Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate at 10 uM in detergent free solution by scintillation counting based radio-TLC assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Assay and inhibition of diacylglycerol lipase activity.
AID458308In vivo inhibition of MAGL in mouse at 20 mg/kg, ip2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID458305Inhibition of NTE in mouse brain membrane at 100 uM2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346214Human acyloxyacyl hydrolase (3.1.1.- Carboxylic Ester Hydrolases)2014Nature chemical biology, Aug, Volume: 10, Issue:8
A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.
AID1345299Human Fatty acid amide hydrolase (Hydrolases)2009Proceedings of the National Academy of Sciences of the United States of America, Dec-01, Volume: 106, Issue:48
Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo.
AID1345301Human Monoacylglycerol lipase (2-Acylglycerol ester turnover)2009Proceedings of the National Academy of Sciences of the United States of America, Dec-01, Volume: 106, Issue:48
Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.86)29.6817
2010's20 (57.14)24.3611
2020's14 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.96

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 Index28.96 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index5.93 (4.65)
Search Engine Demand Index22.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other35 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]