Page last updated: 2024-11-04

prazepam

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Description

Prazepam is a benzodiazepine derivative that acts as a central nervous system depressant. It was initially synthesized in the 1960s and has been studied for its anxiolytic, sedative, hypnotic, and muscle relaxant properties. Prazepam is metabolized into desmethyldiazepam, a long-acting benzodiazepine with a half-life of approximately 100 hours. This slow metabolism contributes to prazepam's long duration of action and potential for accumulation in the body, making it a candidate for long-term treatment of anxiety disorders. Prazepam's efficacy in treating anxiety has been established in clinical trials, but its use has been limited by its side effects, such as drowsiness, dizziness, and impaired coordination. Prazepam is also known to be habit-forming and can lead to dependence. Due to concerns about potential for abuse and its side effect profile, prazepam is not widely prescribed in many countries. However, it remains a valuable tool for the management of certain anxiety disorders when other treatment options have failed.'

Prazepam: A benzodiazepine that is used in the treatment of ANXIETY DISORDERS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4890
CHEMBL ID969
CHEBI ID8362
SCHEMBL ID78272
MeSH IDM0017437

Synonyms (82)

Synonym
2h-1,4-benzodiazepin-2-one, 7-chloro-1-(cyclopropylmethyl)-1,3-dihydro-5-phenyl-
7-chloro-1-(cyclopropylmethyl)-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one
2h-1,4-benzodiazepin-2-one, 1,3-dihydro-7-chloro-1-(cyclopropylmethyl)-5-phenyl-
centrax
prazepamum [inn-latin]
nsc 277179
7-chloro-1-cyclopropylmethyl-5-phenyl-1h-1,4-benzodiazepin-2(3h)-one
7-chloro-1-(cyclopropylmethyl)-1,3-dihydro-5-phenyl-2h-1,4-benzodiazepin-2-one
dea no. 2764
brn 0895797
einecs 220-975-8
7-chloro-1-(cyclopropylmethyl)-1,4-benzodiazepin-2-one
verstran
nsc277179
demetrin
2h-1, 7-chloro-1-(cyclopropylmethyl)-1,3-dihydro-5-phenyl-
wln: t67 gnv jn ihj cg kr& g1- al3tj
nsc-277179
k-373
lysanxia
w 4020
trepidan
2h-1, 1,3-dihydro-7-chloro-1-(cyclopropylmethyl)-5-phenyl-
2955-38-6
prazepam
C07366
DB01588
centrax (tn)
prazepam (jp17/usan/inn)
D00470
NCGC00168256-01
CHEMBL969
w-4020 ,
prazepam civ
chebi:8362 ,
7-chloro-1-(cyclopropylmethyl)-5-phenyl-3h-1,4-benzodiazepin-2-one
NCGC00168256-02
prazepam [usan:usp:inn:ban:jan]
prazepamum
unii-q30vcc064m
q30vcc064m ,
tox21_112615
NCGC00257630-01
dtxsid4021181 ,
tox21_200076
cas-2955-38-6
dtxcid101181
prazene
settima
prazeene
sedapran
smr000058725
MLS003899231
prazepam civ [usp-rs]
prazepam [who-dd]
prazepam [ep monograph]
prazepam [jan]
prazepam [mart.]
prazepam [orange book]
prazepam [usan]
prazepam [vandf]
prazepam [mi]
prazepam [iarc]
prazepam [inn]
gtpl7275
7-chloro-1-(cyclopropylmethyl)-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepin-2-one
SCHEMBL78272
7-chloro-1-(cyclopropylmethyl)-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one #
prazepam, united states pharmacopeia (usp) reference standard
prazepam, european pharmacopoeia (ep) reference standard
prazepam 0.1 mg/ml in methanol
prazepam 1.0 mg/ml in methanol
prazepam 1000 microg/ml in methanol
Q2149443
prazepam civ (usp-rs)
n05ba11
prazepam (iarc)
prazepam (mart.)
prazepam (usan:usp:inn:ban:jan)
prazepamum (inn-latin)
prazepam (ep monograph)
prazepam, 1mg/ml in methanol

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic analysis were carried out by two ways; according to compartmental pharmacokinetic models and by statistic moments."( Pharmacokinetic profiles of prazepam and 14C-prazepam in rat.
Dios-Vieitez, MC; Fos, D; Renedo, MJ, 1991
)
0.58
"The pharmacokinetic profiles of oral and sublingual administrations of prazepam 20 mg to 5 normal volunteers were compared in order to explain the clinical observation that sublingual prazepam appears to exhibit sedative properties when compared to the same dose of oral prazepam."( Comparison of sublingual and oral prazepam in normal subjects. II. Pharmacokinetic and pharmacodynamic data.
Ansseau, M; Jacqmin, P, 1988
)
0.79

Compound-Compound Interactions

ExcerptReferenceRelevance
" The time needed to complete the two-symbol cancellation test was longer when the subjects received prazepam either alone or combined with ethanol."( Comparison of performance of healthy volunteers given prazepam alone or combined with ethanol. Relation to drug plasma concentrations.
Bertaux, L; Fournier, PE; Girre, C; Hirschhorn, M; Palombo, S, 1991
)
0.75

Bioavailability

ExcerptReferenceRelevance
" Simultaneous ingestion of prazepam and ethanol did not alter the bioavailability of either drug."( Comparison of performance of healthy volunteers given prazepam alone or combined with ethanol. Relation to drug plasma concentrations.
Bertaux, L; Fournier, PE; Girre, C; Hirschhorn, M; Palombo, S, 1991
)
0.83
" Thus, differences in absorption rate of orally administered benzodiazepines can lead to differences in the intensity of single-dose effects, despite administration of doses that are equivalent in terms of long-term anxiolytic efficacy."( Plasma concentrations and clinical effects after single oral doses of prazepam, clorazepate, and diazepam.
Allison, S; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Pary, RJ; Shader, RI, 1984
)
0.5
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The anxiolytic activity and tolerance of two dosage schedules of prazepam, a long plasma half-life benzodiazepine, were compared under double-blind conditions. One hundred fifty four patients with DSM III generalized anxiety criteria were included in this study.

ExcerptRelevanceReference
" Demetrin at dosage levels of 3 x 10 mg/day and 3 x 20 mg/day did not influence cardiovascular function."( Effects of Demetrin on circulation.
Kirchhoff, HW, 1975
)
0.25
" One hundred fifty four patients with DSM III generalized anxiety criteria were included in this study and received prazepam at an average dosage of 20 mg per day."( [Prazepam drops versus 10 mg prazepam tablets in anxious patients in ambulatory care].
Chabannes, JP; Lemoine, P,
)
1.25
" The equipotent dosage to 10 mg prazepam seems to be 5 mg."( Classification and assessment of cerebral bioavailability of lopirazepam (D-12524) by quantitative EEG and psychometric analysis.
Grünberger, J; Linzmayer, L; Saletu, B; Stadler, R, 1980
)
0.54
"The anxiolytic activity and tolerance of two dosage schedules of prazepam, a long plasma half-life benzodiazepine, were compared under double-blind conditions in two groups of 10 inpatients each who met Research Diagnostic Criteria for Generalized Anxiety Disorder and presented chronic and severe symptomatology."( Duration of benzodiazepine clinical activity: lack of direct relationship with plasma half-life. A comparison of single vs divided dosage schedules of prazepam.
Ansseau, M; Collard, J; Doumont, A; von Frenckell, R, 1984
)
0.7
" This was also reflected in the spectral analyzed EEG, which showed, after one single dosage of both drugs, a typical anxiolytic profile which was more pronounced after lopirazepam than prazepam, while after the chronic administration (12 h after the evening medication) only prazepam showed an anxiolytic profile."( Clinical symptomatology and computer analyzed EEG before, during and after anxiolytic therapy of alcohol withdrawal patients.
Grünberger, J; Karobath, M; Mader, R; Saletu, B; Saletu, M, 1983
)
0.46
" Patients were allocated at random to receive 30 mg prazepam or 15 mg diazepam per day, either in divided dosage (3 times) during the day or as a single large dose at night."( A multi-centre comparison of prazepam and diazepam in the treatment of anxiety.
Dorman, T, 1983
)
0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzodiazepineA group of heterocyclic compounds with a core structure containing a benzene ring fused to a diazepine ring.
[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 (23)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency52.10480.002541.796015,848.9004AID1347397; AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency50.95620.006038.004119,952.5996AID1159523
USP1 protein, partialHomo sapiens (human)Potency70.79460.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency28.60660.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency50.95620.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency44.99300.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency28.65480.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency56.10770.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency11.40770.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.77830.01237.983543.2770AID1346984
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency45.80840.000214.376460.0339AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency40.82680.000817.505159.3239AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency41.58510.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency40.31400.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency13.76700.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency40.98730.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743080; AID743091
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency11.22020.10009.191631.6228AID1346983
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency37.79460.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency37.51270.000627.21521,122.0200AID743202; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency22.79360.005612.367736.1254AID624032
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency45.41480.001557.789015,848.9004AID1259244
Cellular tumor antigen p53Homo sapiens (human)Potency44.39370.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency45.41480.001551.739315,848.9004AID1259244
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID227697Compound was evaluated for the Anti-fighting behavior.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID227698Evaluation for the Anti-pentylenetetrazole effect.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID113676Effect on hexobarbital induced sleep was determined in hexobarbital potentiation test; Range (8.3-15.4)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
AID114460Ataxic activity in mice by rotarod test; Range (1.1-5.3)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
AID599144Intrinsic solubility, log 1/S0 of the compound2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Computational aqueous solubility prediction for drug-like compounds in congeneric series.
AID194131ED50 value was reported as log1/C, which is the concentration required to reduce locomotor activity by 50% in rats1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID235587Ratio of ED50 (hexobarbital) to that of ED50 (fighting)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
AID23479Partition coefficient (logP)1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID235588Ratio of ED50 (rotarod) to that of ED50 (fighting)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
AID1660982Inhibition of Escherichia coli Stx2 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation at 30 uM incubated with cells for 4 hrs prior to Stx2 addition and further incubated for 20 hrs and s2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
AID113281Antiaggressive anxiolytic activity in the electroshock-induced fighting test in mice (po); Range (6.62-10.07)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
AID228469Evaluation of inclined screen test.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (112)

TimeframeStudies, This Drug (%)All Drugs %
pre-199079 (70.54)18.7374
1990's16 (14.29)18.2507
2000's12 (10.71)29.6817
2010's3 (2.68)24.3611
2020's2 (1.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 77.00

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index77.00 (24.57)
Research Supply Index5.11 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index134.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (77.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials36 (28.13%)5.53%
Reviews6 (4.69%)6.00%
Case Studies10 (7.81%)4.05%
Observational0 (0.00%)0.25%
Other76 (59.38%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]