Compounds > N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-2-naphthalenecarboxamide
Page last updated: 2024-11-13

N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-2-naphthalenecarboxamide

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

Cross-References

ID SourceID
PubMed CID25105704
CHEMBL ID492797
CHEBI ID131157
SCHEMBL ID2724877

Synonyms (25)

Synonym
n-(2-(4-(2-oxo-2,3-dihydro-1h-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-2-naphthamide
CHEMBL492797 ,
CHEBI:131157
VU0155056-3
VU0155056-1
VU0155056-2 ,
ml272
SCHEMBL2724877
bdbm87245
n-[2-[4-(2-oxo-3h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-2-naphthalenecarboxamide;hydrochloride
n-(2-(4-(2-oxo-2,3-dihydro-1h-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-2-naphthamide, 56
n-[2-[4-(2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]ethyl]naphthalene-2-carboxamide;hydrochloride
n-[2-[4-(2-keto-3h-benzimidazol-1-yl)piperidino]ethyl]-2-naphthamide;hydrochloride
us9453017, 3
vu0156056 (1)
n-[2-[4-(2-oxidanylidene-3h-benzimidazol-1-yl)piperidin-1-yl]ethyl]naphthalene-2-carboxamide;hydrochloride
n-(2-{4-[2-oxo-2,3-dihydro-1h-benzo(d)imidazol-1-yl]piperidin-1-yl}ethyl)-2-naphthamide (inh_vu0155056)
cid_53481919
1130067-18-3
n-{2-[4-(2-oxo-2,3-dihydro-1h-1,3-benzodiazol-1-yl)piperidin-1-yl]ethyl}naphthalene-2-carboxamide
NCGC00386898-01
Q27224941
n-[2-[4-(2-oxo-3h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-2-naphthalenecarboxamide
n-[2-[4-(2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]ethyl]naphthalene-2-carboxamide
n-(2-{4-[2-oxo-2,3-dihydro-1h-benzo(d)imidazol-1-yl]piperidin-1-yl}ethyl)-2-naphthamide

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
naphthalenecarboxamideAny member of the class of naphthalenes in which the naphthalene ring is directly attached to the carbonyl carbon of a carboxamide group.
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.11160.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency7.56370.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency11.98770.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency7.56370.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
[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)
Phospholipase D2Homo sapiens (human)IC50 (µMol)0.23230.00611.159810.0000AID1800492; AID1801138; AID418767; AID498478; AID498482
Phospholipase D1 Rattus norvegicus (Norway rat)IC50 (µMol)1.00000.01100.34381.0000AID498481
Phospholipase D1Homo sapiens (human)IC50 (µMol)0.20700.00101.06568.5000AID1799395; AID1799396; AID1799399; AID1800492; AID1801138; AID418766; AID498477; AID498484
[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)
Phospholipase D1Homo sapiens (human)EC50 (µMol)0.20050.00101.23098.5000AID1799397; AID1799398
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (58)

Processvia Protein(s)Taxonomy
phosphatidic acid biosynthetic processPhospholipase D2Homo sapiens (human)
cytoskeleton organizationPhospholipase D2Homo sapiens (human)
small GTPase-mediated signal transductionPhospholipase D2Homo sapiens (human)
synaptic vesicle recyclingPhospholipase D2Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisPhospholipase D2Homo sapiens (human)
phospholipid catabolic processPhospholipase D2Homo sapiens (human)
regulation of vesicle-mediated transportPhospholipase D2Homo 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)
phosphatidic acid biosynthetic processPhospholipase D1Homo sapiens (human)
chemotaxisPhospholipase D1Homo sapiens (human)
small GTPase-mediated signal transductionPhospholipase D1Homo sapiens (human)
Ras protein signal transductionPhospholipase D1Homo sapiens (human)
cellular response to nutrientPhospholipase D1Homo sapiens (human)
regulation of microvillus assemblyPhospholipase D1Homo sapiens (human)
positive regulation of translationPhospholipase D1Homo sapiens (human)
regulation of synaptic vesicle cyclePhospholipase D1Homo sapiens (human)
phospholipid catabolic processPhospholipase D1Homo sapiens (human)
regulation of vesicle-mediated transportPhospholipase D1Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
phospholipase D activityPhospholipase D2Homo sapiens (human)
protein bindingPhospholipase D2Homo sapiens (human)
phosphatidylinositol bindingPhospholipase D2Homo sapiens (human)
N-acylphosphatidylethanolamine-specific phospholipase D activityPhospholipase D2Homo 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)
phospholipase D activityPhospholipase D1Homo sapiens (human)
protein bindingPhospholipase D1Homo sapiens (human)
phosphatidylinositol bindingPhospholipase D1Homo sapiens (human)
N-acylphosphatidylethanolamine-specific phospholipase D activityPhospholipase D1Homo 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 (35)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membranePhospholipase D2Homo sapiens (human)
plasma membranePhospholipase D2Homo sapiens (human)
presynapsePhospholipase D2Homo sapiens (human)
intracellular membrane-bounded organellePhospholipase D2Homo sapiens (human)
plasma membrane regionPhospholipase D2Homo 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)
cholinergic synapsePhospholipase D1Homo sapiens (human)
Golgi membranePhospholipase D1Homo sapiens (human)
lysosomal membranePhospholipase D1Homo sapiens (human)
endosomePhospholipase D1Homo sapiens (human)
endoplasmic reticulum membranePhospholipase D1Homo sapiens (human)
Golgi apparatusPhospholipase D1Homo sapiens (human)
plasma membranePhospholipase D1Homo sapiens (human)
membranePhospholipase D1Homo sapiens (human)
apical plasma membranePhospholipase D1Homo sapiens (human)
endocytic vesiclePhospholipase D1Homo sapiens (human)
late endosome membranePhospholipase D1Homo sapiens (human)
specific granule membranePhospholipase D1Homo sapiens (human)
perinuclear region of cytoplasmPhospholipase D1Homo sapiens (human)
tertiary granule membranePhospholipase D1Homo sapiens (human)
intracellular membrane-bounded organellePhospholipase D1Homo sapiens (human)
plasma membrane regionPhospholipase D1Homo 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 (29)

Assay IDTitleYearJournalArticle
AID1799398293-PLD2 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799399PLD2 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799395PLD1 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1801138In vivo Deuterated 1-Butanol PLD Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\2015ACS chemical biology, Feb-20, Volume: 10, Issue:2
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.
AID1801141Exogenous PldA Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\2015ACS chemical biology, Feb-20, Volume: 10, Issue:2
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.
AID1800492PLD In Vitro Kinetic Assay from Article 10.1111/cbdd.12319: \\1,3-disubstituted-4-aminopyrazolo [3, 4-d] pyrimidines, a new class of potent inhibitors for phospholipase D.\\2014Chemical biology & drug design, Sep, Volume: 84, Issue:3
1,3-disubstituted-4-aminopyrazolo [3, 4-d] pyrimidines, a new class of potent inhibitors for phospholipase D.
AID1799396d.311 Enzymatic Inhibition Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799397Calu-1 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498471Inhibition of PLD2 mediated cancer cell migration in mouse PMT cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID418768Selectivity for human PLD1 over human PLD22009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
AID498476Inhibition of PLD1 mediated cancer cell migration in human MDA-231 cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498472Inhibition of PLD2 mediated cancer cell migration in mouse 4T1 cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498474Inhibition of PLD1 mediated cancer cell migration in mouse 4T1 cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498477Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498473Inhibition of PLD2 mediated cancer cell migration in human MDA-231 cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID349540Selectivity for PLD1 in human Calu1 cells over GFP-labeled PLD2 in human HEK293 cells2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
AID418767Inhibition of GFP-labelled human PLD2 HEK293 cells2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
AID498478Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498283Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins stimulated with myr-Arf-12009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498481Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498475Inhibition of PLD1 mediated cancer cell migration in mouse PMT cells at 20 uM by transwell invasion assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID418766Inhibition of human PLD1 in Calu1 cells2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
AID498484Inhibition of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498482Inhibition of human PLD2 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (37.50)29.6817
2010's3 (37.50)24.3611
2020's2 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.47

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 Index12.47 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.47)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
1-NA-PP1
[no description available]		2.110pyrazolopyrimidinetyrosine kinase inhibitor
raloxifene
raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.		2.48201-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols		bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
[no description available]		2.0510stilbenoid
halopemide
halopemide: structure		2.4520
1-(4-pyridyl)piperazine
1-(4-pyridyl)piperazine: structure in first source		2.0510
1-(2-pyridinyl)piperazine
1-(2-pyridinyl)piperazine: metabolite of buspirone & gepirone		2.0510
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.0510resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
diethylstilbestrol
Diethylstilbestrol: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed). diethylstilbestrol : An olefinic compound that is trans-hex-3-ene in which the hydrogens at positions 3 and 4 have been replaced by p-hydroxyphenyl groups.		2.0510olefinic compound;
polyphenol		antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen
afimoxifene
afimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.		2.1110phenols;
tertiary amino compound		antineoplastic agent;
estrogen receptor antagonist;
metabolite
tamoxifen
[no description available]		2.4820stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
5-fluoro-2-indolyldeschlorohalopemide
[no description available]		2.4720benzimidazoles
vu0155069
[no description available]		2.4520
ml298
[no description available]		2.1110
ml299
ML299: has antineoplastic activity; structure in first source		2.1110
ConditionIndicatedRelationship StrengthStudiesTrials
Breast Cancer
[description not available]		02.0510
Invasiveness, Neoplasm
[description not available]		02.0510
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.0510
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510