Page last updated: 2024-12-10

jnj-1661010

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Cross-References

ID SourceID
PubMed CID2809273
CHEMBL ID460273
CHEBI ID192640
SCHEMBL ID1164398
MeSH IDM0528591

Synonyms (40)

Synonym
n1-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
MLS001111246
smr000458006
OPREA1_746619
bdbm50244718
cid_2809273
HMS1662H10
CHEMBL460273 ,
CHEBI:192640
jnj-1661010
n-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
681136-29-8
1-piperazinecarboxamide, n-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-
HMS2801K13
jnj 1661010
62521s57au ,
unii-62521s57au
S2828
jnj1661010
gtpl5206
SCHEMBL1164398
BHBOSTKQCZEAJM-UHFFFAOYSA-N ,
n-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-1-piperazinecarboxamide
AC-32902
AKOS024457512
DTXSID00384599
takeda-25
jnj-1661010, >=98% (hplc)
HMS3651L15
AS-72170
NCGC00378802-04
SW220165-1
BCP06935
Q27894028
EX-A2218
SB19582
CCG-268230
CS-0003322
HY-N7062
A899884

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]

Drug Classes (1)

ClassDescription
N-arylpiperazine
[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 (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency10.00000.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency23.09990.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency19.73470.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.50920.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency5.35470.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.10930.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency31.62283.548119.542744.6684AID743266
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
VprHuman immunodeficiency virus 1Potency63.09571.584919.626463.0957AID651644
Interferon betaHomo sapiens (human)Potency5.35470.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.48131.995325.532750.1187AID624288
TAR DNA-binding protein 43Homo sapiens (human)Potency11.22021.778316.208135.4813AID652104
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
[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)
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC50 (µMol)20.00000.873010.721978.4000AID493155
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50 (µMol)0.02960.00020.59827.0000AID363657; AID363659; AID363660; AID363661; AID430491; AID612783; AID726794
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.02600.00051.33138.0000AID363656; AID590552; AID612777
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
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 (33)

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)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
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
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)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
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 (66)

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.
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.
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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID363685Tmax in rat brain at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363682Cmax in rat plasma at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID430491Inhibition of FAAH2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
AID363688Increase in anandamide levels in rat brain at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363687Ex vivo inhibition of FAAH in rat brain at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363659Inhibition of human FAAH preincubated for 10 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363667Clearance in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID612783Inhibition of FAAH2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
AID363678Half life in rat plasma at 1 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363668Volume of distribution in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363679Mean retention time in rat at 1 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363675Volume of distribution in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363660Inhibition of human FAAH after 60 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363662Inhibition of rat liver esterase assessed as ester (4-nitrophenyl-acetate) hydrolysis at 10 uM after 30 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID590552Inhibition of rat FAAH assessed as hydrolysis of anandamido-amino-methyl-cumarin2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
AID363672Half life in rat plasma at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363674Clearance in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363669Oral bioavailability in rat at 10 mg/kg2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363690Inhibition of rat FAAH assessed as recovery of enzyme activity at IC80 concentration after 18 hrs at 22 degC by dialysis2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363689Inhibition of rat FAAH assessed as recovery of enzyme activity at IC80 concentration after 18 hrs at 4 degC by dialysis2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363656Inhibition of rat FAAH preincubated for 20 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363657Inhibition of human FAAH preincubated for 20 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363663Cmax in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363684Cmax in rat brain at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363664Tmax in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363671Tmax in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363665Half life in rat plasma at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363692Increase in anandamide levels in rat brain at 20 mg/kg, ip after 4 hrs relative to control2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363666Mean retention time in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363661Inhibition of human FAAH preincubated for 40 mins2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363676Bioavailability in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363670Cmax in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363683Tmax in rat plasma at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363681Volume of distribution in rat at 1 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363680Clearance in rat at 1 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363691Ex vivo inhibition of FAAH in rat brain assessed as recovered enzyme activity at 20 mg/kg, ip after 24 hrs relative to control2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363673Mean retention time in rat at 10 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID363677Cmax in rat at 1 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID726794Apparent inhibition of human FAAH expressed in CHO-K1 cells using ethanolamine 1-3[H] as substrate after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.
AID612777Inhibition of rat FAAH2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
AID1298618Reversible inhibition of MBP-fused human recombinant FAAH with truncated N-terminal transmembrane domain expressed in Escherichia coli T7 assessed as enzyme activity recovery rate using D-AMC substrate measured 24 to 144 hrs after exhaustive dialysis by f2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Piperidinyl thiazole isoxazolines: A new series of highly potent, slowly reversible FAAH inhibitors with analgesic properties.
AID363686Blood-brain barrier coefficient in rat assessed as log of ratio of brain AUC to plasma AUC at 20 mg/kg, ip2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID1345299Human Fatty acid amide hydrolase (Hydrolases)2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
AID1345254Human Fatty acid amide hydrolase-2 (N-Acylethanolamine turnover)2009Anesthesia and analgesia, Jan, Volume: 108, Issue:1
Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (21.05)29.6817
2010's11 (57.89)24.3611
2020's4 (21.05)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.73

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 Index16.73 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (94.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]