halopemide profile

halopemide: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	65490
CHEMBL ID	245621
SCHEMBL ID	121267
MeSH ID	M0068079

Synonym
n-[2-[4-(5-chloro-2-oxo-1-benzimidazolinyl)piperidino]ethyl]-p-fluorobenzamide
benzamide,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluoro-
halopemide
mls003171133 ,
59831-65-1
r 34,301
nsc354856
nsc-354856
D02665
halopemide (usan/inn)
r-34301
CHEMBL245621 ,
n-[2-[4-(5-chloro-2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]ethyl]-4-fluorobenzamide
cid_65490
bdbm50206160
halopemide, 8
n-(2-(4-(5-chloro-2-oxo-2,3-dihydro-1h-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-4-fluorobenzamide ,
n-(2-(4-(5-chloro-2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-4-fluorobenzamide
smr001875041
n-(2-(4-(5-chlor-2,3-dihydro-2-oxo-1-benzimidazolyl)piperidino)ethyl)-4-fluorbenzamid
r 34301
nsc 354856
halopemidum
halopemida [inn-spanish]
benzamide, n-(2-(4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)ethyl)-4-fluoro-
65q28tv0zy ,
unii-65q28tv0zy
halopemida
halopemide [usan:inn]
halopemidum [inn-latin]
n-(2-(4-(5-chloro-2-oxo-1-benzimidazolinyl)piperidino)ethyl)-p-fluorobenzamide
VU0155067-2
halopemide [inn]
halopemide [usan]
SCHEMBL121267
MLS006012046
smr002529688
n-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluorobenzamide
NBHPRWLFLUBAIE-UHFFFAOYSA-N
HMS3648G20
DTXSID20208561
halopemide, >=98% (hplc)
MJV ,
n-{2-[4-(5-chloro-2-oxo-2,3-dihydro-1h-benzimidazol-1-yl)piperidin-1-yl]ethyl}-4-fluorobenzamide
HY-119093
CS-0067969
sr-01000946369
SR-01000946369-1
Q27263902
n-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]-ethyl]-4-fluoro-benzamide
MS-27272
AKOS040741828

Excerpt	Reference	Relevance
"Halopemide is a new psychotropic agent, structurally related to the neuroleptics of the butyrophenone type, but with a different phamacological and clinical profile. "	( Regional localization of halopemide, a new psychotropic agent, in the rat brain. Janssen, PA; Loonen, AJ; Soudijn, W; van Wijngaarden, I, 1978)	2
"Halopemide is a new psychotropic agent, a structural analogue of the neuroleptics of the butyrophenone type but with different pharmacological and clinical properties. "	( Halopemide, a new psychotropic agent. Cerebral distribution and receptor interactions. Loonen, AJ; Soudijn, W, 1985)	3.15

Excerpt	Relevance	Reference
" Repeated early morning trough measures of plasma clozapine and prolactin levels on each subject were studied during the course of a double-blind dose-response clozapine study."	( Possible individual and gender differences in the small increases in plasma prolactin levels seen during clozapine treatment. de Leon, J; Diaz, FJ; Josiassen, RC; Simpson, GM, 2004)	0.32

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
phospholipase D1 isoform b	Homo sapiens (human)	IC50 (µMol)	0.0080	0.0080	0.0080	0.0080	AID602151
phospholipase D2 isoform PLD2B	Homo sapiens (human)	IC50 (µMol)	0.2800	0.2800	0.2800	0.2800	AID602147
phospholipase D1 isoform a [Homo sapiens]	Homo sapiens (human)	IC50 (µMol)	0.0080	0.0080	0.0080	0.0080	AID602151
phospholipase D2 isoform PLD2A	Homo sapiens (human)	IC50 (µMol)	0.2800	0.2800	0.2800	0.2800	AID602147
Phospholipase D2	Homo sapiens (human)	IC50 (µMol)	1.5367	0.0061	1.1598	10.0000	AID1532921; AID306650; AID418767; AID498478; AID498482; AID729472
D(2) dopamine receptor	Homo sapiens (human)	IC50 (µMol)	0.0070	0.0000	0.7472	8.0000	AID729471
Phospholipase D1	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0110	0.0110	0.3438	1.0000	AID498481
Phospholipase D1	Homo sapiens (human)	IC50 (µMol)	0.1305	0.0010	1.0656	8.5000	AID1532920; AID1799395; AID1799396; AID1799399; AID418766; AID498477; AID498484; AID729469
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Phospholipase D1	Homo sapiens (human)	EC50 (µMol)	0.1605	0.0010	1.2309	8.5000	AID1799397; AID1799398
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
phosphatidic acid biosynthetic process	Phospholipase D2	Homo sapiens (human)
cytoskeleton organization	Phospholipase D2	Homo sapiens (human)
small GTPase-mediated signal transduction	Phospholipase D2	Homo sapiens (human)
synaptic vesicle recycling	Phospholipase D2	Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosis	Phospholipase D2	Homo sapiens (human)
phospholipid catabolic process	Phospholipase D2	Homo sapiens (human)
regulation of vesicle-mediated transport	Phospholipase D2	Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
temperature homeostasis	D(2) dopamine receptor	Homo sapiens (human)
response to hypoxia	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of protein phosphorylation	D(2) dopamine receptor	Homo sapiens (human)
response to amphetamine	D(2) dopamine receptor	Homo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressure	D(2) dopamine receptor	Homo sapiens (human)
regulation of heart rate	D(2) dopamine receptor	Homo sapiens (human)
regulation of sodium ion transport	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor internalization	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of neuroblast proliferation	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of receptor internalization	D(2) dopamine receptor	Homo sapiens (human)
autophagy	D(2) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
neuron-neuron synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
neuroblast proliferation	D(2) dopamine receptor	Homo sapiens (human)
axonogenesis	D(2) dopamine receptor	Homo sapiens (human)
synapse assembly	D(2) dopamine receptor	Homo sapiens (human)
sensory perception of smell	D(2) dopamine receptor	Homo sapiens (human)
long-term memory	D(2) dopamine receptor	Homo sapiens (human)
grooming behavior	D(2) dopamine receptor	Homo sapiens (human)
locomotory behavior	D(2) dopamine receptor	Homo sapiens (human)
adult walking behavior	D(2) dopamine receptor	Homo sapiens (human)
protein localization	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cell population proliferation	D(2) dopamine receptor	Homo sapiens (human)
associative learning	D(2) dopamine receptor	Homo sapiens (human)
visual learning	D(2) dopamine receptor	Homo sapiens (human)
response to xenobiotic stimulus	D(2) dopamine receptor	Homo sapiens (human)
response to light stimulus	D(2) dopamine receptor	Homo sapiens (human)
response to toxic substance	D(2) dopamine receptor	Homo sapiens (human)
response to iron ion	D(2) dopamine receptor	Homo sapiens (human)
response to inactivity	D(2) dopamine receptor	Homo sapiens (human)
Wnt signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
striatum development	D(2) dopamine receptor	Homo sapiens (human)
orbitofrontal cortex development	D(2) dopamine receptor	Homo sapiens (human)
cerebral cortex GABAergic interneuron migration	D(2) dopamine receptor	Homo sapiens (human)
adenohypophysis development	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cell migration	D(2) dopamine receptor	Homo sapiens (human)
peristalsis	D(2) dopamine receptor	Homo sapiens (human)
auditory behavior	D(2) dopamine receptor	Homo sapiens (human)
regulation of synaptic transmission, GABAergic	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of cytokinesis	D(2) dopamine receptor	Homo sapiens (human)
circadian regulation of gene expression	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of dopamine secretion	D(2) dopamine receptor	Homo sapiens (human)
response to histamine	D(2) dopamine receptor	Homo sapiens (human)
response to nicotine	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of urine volume	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of renal sodium excretion	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of multicellular organism growth	D(2) dopamine receptor	Homo sapiens (human)
response to cocaine	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleep	D(2) dopamine receptor	Homo sapiens (human)
dopamine metabolic process	D(2) dopamine receptor	Homo sapiens (human)
drinking behavior	D(2) dopamine receptor	Homo sapiens (human)
regulation of potassium ion transport	D(2) dopamine receptor	Homo sapiens (human)
response to morphine	D(2) dopamine receptor	Homo sapiens (human)
pigmentation	D(2) dopamine receptor	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of blood pressure	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of innate immune response	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of insulin secretion	D(2) dopamine receptor	Homo sapiens (human)
acid secretion	D(2) dopamine receptor	Homo sapiens (human)
behavioral response to cocaine	D(2) dopamine receptor	Homo sapiens (human)
behavioral response to ethanol	D(2) dopamine receptor	Homo sapiens (human)
regulation of long-term neuronal synaptic plasticity	D(2) dopamine receptor	Homo sapiens (human)
response to axon injury	D(2) dopamine receptor	Homo sapiens (human)
branching morphogenesis of a nerve	D(2) dopamine receptor	Homo sapiens (human)
arachidonic acid secretion	D(2) dopamine receptor	Homo sapiens (human)
epithelial cell proliferation	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of epithelial cell proliferation	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of protein secretion	D(2) dopamine receptor	Homo sapiens (human)
release of sequestered calcium ion into cytosol	D(2) dopamine receptor	Homo sapiens (human)
dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
regulation of dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
regulation of synapse structural plasticity	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	D(2) dopamine receptor	Homo sapiens (human)
excitatory postsynaptic potential	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of growth hormone secretion	D(2) dopamine receptor	Homo sapiens (human)
prepulse inhibition	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	D(2) dopamine receptor	Homo sapiens (human)
regulation of locomotion involved in locomotory behavior	D(2) dopamine receptor	Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cellular response to hypoxia	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor production	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	D(2) dopamine receptor	Homo sapiens (human)
hyaloid vascular plexus regression	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of neuron migration	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cytosolic calcium ion concentration	D(2) dopamine receptor	Homo sapiens (human)
regulation of dopamine secretion	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of adenylate cyclase activity	D(2) dopamine receptor	Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of voltage-gated calcium channel activity	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of MAPK cascade	D(2) dopamine receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
phosphatidic acid biosynthetic process	Phospholipase D1	Homo sapiens (human)
chemotaxis	Phospholipase D1	Homo sapiens (human)
small GTPase-mediated signal transduction	Phospholipase D1	Homo sapiens (human)
Ras protein signal transduction	Phospholipase D1	Homo sapiens (human)
cellular response to nutrient	Phospholipase D1	Homo sapiens (human)
regulation of microvillus assembly	Phospholipase D1	Homo sapiens (human)
positive regulation of translation	Phospholipase D1	Homo sapiens (human)
regulation of synaptic vesicle cycle	Phospholipase D1	Homo sapiens (human)
phospholipid catabolic process	Phospholipase D1	Homo sapiens (human)
regulation of vesicle-mediated transport	Phospholipase D1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
phospholipase D activity	Phospholipase D2	Homo sapiens (human)
protein binding	Phospholipase D2	Homo sapiens (human)
phosphatidylinositol binding	Phospholipase D2	Homo sapiens (human)
N-acylphosphatidylethanolamine-specific phospholipase D activity	Phospholipase D2	Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/Go	D(2) dopamine receptor	Homo sapiens (human)
G-protein alpha-subunit binding	D(2) dopamine receptor	Homo sapiens (human)
protein binding	D(2) dopamine receptor	Homo sapiens (human)
heterotrimeric G-protein binding	D(2) dopamine receptor	Homo sapiens (human)
dopamine binding	D(2) dopamine receptor	Homo sapiens (human)
ionotropic glutamate receptor binding	D(2) dopamine receptor	Homo sapiens (human)
identical protein binding	D(2) dopamine receptor	Homo sapiens (human)
heterocyclic compound binding	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor activity	D(2) dopamine receptor	Homo sapiens (human)
phospholipase D activity	Phospholipase D1	Homo sapiens (human)
protein binding	Phospholipase D1	Homo sapiens (human)
phosphatidylinositol binding	Phospholipase D1	Homo sapiens (human)
N-acylphosphatidylethanolamine-specific phospholipase D activity	Phospholipase D1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endoplasmic reticulum membrane	Phospholipase D2	Homo sapiens (human)
plasma membrane	Phospholipase D2	Homo sapiens (human)
presynapse	Phospholipase D2	Homo sapiens (human)
intracellular membrane-bounded organelle	Phospholipase D2	Homo sapiens (human)
plasma membrane region	Phospholipase D2	Homo sapiens (human)
Golgi membrane	D(2) dopamine receptor	Homo sapiens (human)
acrosomal vesicle	D(2) dopamine receptor	Homo sapiens (human)
plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
cilium	D(2) dopamine receptor	Homo sapiens (human)
lateral plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
endocytic vesicle	D(2) dopamine receptor	Homo sapiens (human)
axon	D(2) dopamine receptor	Homo sapiens (human)
dendrite	D(2) dopamine receptor	Homo sapiens (human)
synaptic vesicle membrane	D(2) dopamine receptor	Homo sapiens (human)
sperm flagellum	D(2) dopamine receptor	Homo sapiens (human)
dendritic spine	D(2) dopamine receptor	Homo sapiens (human)
perikaryon	D(2) dopamine receptor	Homo sapiens (human)
axon terminus	D(2) dopamine receptor	Homo sapiens (human)
postsynaptic membrane	D(2) dopamine receptor	Homo sapiens (human)
ciliary membrane	D(2) dopamine receptor	Homo sapiens (human)
non-motile cilium	D(2) dopamine receptor	Homo sapiens (human)
dopaminergic synapse	D(2) dopamine receptor	Homo sapiens (human)
GABA-ergic synapse	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor complex	D(2) dopamine receptor	Homo sapiens (human)
glutamatergic synapse	D(2) dopamine receptor	Homo sapiens (human)
presynaptic membrane	D(2) dopamine receptor	Homo sapiens (human)
plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
cholinergic synapse	Phospholipase D1	Homo sapiens (human)
Golgi membrane	Phospholipase D1	Homo sapiens (human)
lysosomal membrane	Phospholipase D1	Homo sapiens (human)
endosome	Phospholipase D1	Homo sapiens (human)
endoplasmic reticulum membrane	Phospholipase D1	Homo sapiens (human)
Golgi apparatus	Phospholipase D1	Homo sapiens (human)
plasma membrane	Phospholipase D1	Homo sapiens (human)
membrane	Phospholipase D1	Homo sapiens (human)
apical plasma membrane	Phospholipase D1	Homo sapiens (human)
endocytic vesicle	Phospholipase D1	Homo sapiens (human)
late endosome membrane	Phospholipase D1	Homo sapiens (human)
specific granule membrane	Phospholipase D1	Homo sapiens (human)
perinuclear region of cytoplasm	Phospholipase D1	Homo sapiens (human)
tertiary granule membrane	Phospholipase D1	Homo sapiens (human)
intracellular membrane-bounded organelle	Phospholipase D1	Homo sapiens (human)
plasma membrane region	Phospholipase D1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay ID	Title	Year	Journal	Article
AID1799398	293-PLD2 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799397	Calu-1 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799395	PLD1 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799396	d.311 Enzymatic Inhibition Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1799399	PLD2 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498481	Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID729472	Inhibition of PLD2 (unknown origin)	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID418766	Inhibition of human PLD1 in Calu1 cells	2009	Bioorganic & 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.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID729469	Inhibition of PLD1 (unknown origin)	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID498477	Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1532920	Inhibition of PLD1 (unknown origin)
AID1532921	Inhibition of PLD2 (unknown origin)
AID498484	Inhibition of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID498478	Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID306650	Inhibition of PLD2	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Optimization of halopemide for phospholipase D2 inhibition.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID498482	Inhibition of human PLD2 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay	2009	Nature chemical biology, Feb, Volume: 5, Issue:2	Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID418767	Inhibition of GFP-labelled human PLD2 HEK293 cells	2009	Bioorganic & 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.
AID729471	Inhibition of dopamine receptor D2 (unknown origin)	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID418768	Selectivity for human PLD1 over human PLD2	2009	Bioorganic & 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	12 (63.16)	18.7374
1990's	0 (0.00)	18.2507
2000's	5 (26.32)	29.6817
2010's	2 (10.53)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (10.00%)	5.53%
Reviews	1 (5.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	17 (85.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.	2.36	2	0	amino acid zwitterion; gamma-amino acid; monocarboxylic acid	human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule
diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.	1.96	1	0	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic
domperidone Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.	7.09	15	2	benzimidazoles; heteroarylpiperidine	antiemetic; dopaminergic antagonist
flunitrazepam Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia.	1.96	1	0	1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes	anxiolytic drug; GABAA receptor agonist; sedative
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	2.36	2	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
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.	2.05	1	0	1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols	bone density conservation agent; estrogen antagonist; estrogen receptor modulator
spiperone Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.	1.95	1	0	aromatic ketone; azaspiro compound; organofluorine compound; piperidines; tertiary amino compound	alpha-adrenergic antagonist; antipsychotic agent; dopaminergic antagonist; psychotropic drug; serotonergic antagonist
sulpiride Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.	1.96	1	0	benzamides; N-alkylpyrrolidine; sulfonamide	antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist
apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.	2.65	3	0	aporphine alkaloid	alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug
pimozide Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.	1.95	1	0	benzimidazoles; heteroarylpiperidine; organofluorine compound	antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist
bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.	1.96	1	0	indole alkaloid	antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol [no description available]	2.05	1	0	stilbenoid
oxiperomide oxiperomide: dopamine-blocking agent	6.96	1	0
mezilamine mezilamine: RN given refers to parent cpd; synonym O 6553 refers to HCl; structure	6.96	1	0
resveratrol trans-resveratrol : A resveratrol in which the double bond has E configuration.	2.05	1	0	resveratrol	antioxidant; 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.	2.05	1	0	olefinic 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
tamoxifen [no description available]	2.05	1	0	stilbenoid; 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
tiapamil hydrochloride Tiapamil Hydrochloride: A phenylethylamine derivative that acts as a calcium antagonist showing hemodynamic effects in patients with acute myocardial infarction.	1.96	1	0
gastrins Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.	1.97	1	0
5-fluoro-2-indolyldeschlorohalopemide [no description available]	2.44	2	0	benzimidazoles
N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-2-naphthalenecarboxamide [no description available]	2.45	2	0	naphthalenecarboxamide
vu0155069 [no description available]	2.45	2	0
piperidines Piperidines: A family of hexahydropyridines.	3.05	5	0
ml298 [no description available]	2.08	1	0
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	3.4	1	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic

Condition	Relationship Strength	Studies	Trials
Breast Cancer [description not available]	2.05	1	0
Invasiveness, Neoplasm [description not available]	2.47	2	0
Breast Neoplasms Tumors or cancer of the human BREAST.	2.05	1	0
Astrocytoma, Grade IV [description not available]	2.08	1	0
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	2.08	1	0
Dementia Praecox [description not available]	3.4	1	1
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	3.4	1	1
Behavior Disorders [description not available]	3.35	1	1
Mental Disorders Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function.	3.35	1	1
Dyskinesia, Medication-Induced [description not available]	3.28	2	0
Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)	3.28	2	0
Emesis [description not available]	1.97	1	0
Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH.	1.97	1	0
Psychoses [description not available]	2.88	1	0
Psychotic Disorders Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994)	2.88	1	0

halopemide

Description

Cross-References

Synonyms (52)

Research Excerpts

Overview

Dosage Studied

Protein Targets (8)

Inhibition Measurements

Activation Measurements

Biological Processes (110)

Molecular Functions (12)

Ceullar Components (35)

Bioassays (38)

Research

Studies (19)

Market Indicators

Research Demand Index: 18.54

Study Types

halopemide

Description

Cross-References

Synonyms (52)

Research Excerpts

Overview

Dosage Studied

Protein Targets (8)

Inhibition Measurements

Activation Measurements

Biological Processes (110)

Molecular Functions (12)

Ceullar Components (35)

Bioassays (38)

Research

Studies (19)

Market Indicators

Research Demand Index: 18.54

Study Types

Related Drugs (25)

Related Conditions (15)