Page last updated: 2024-11-09

benzotript

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

Description

benzotript: anti-gastrinic; active group is amide; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2060890
CHEMBL ID63544
SCHEMBL ID93960
MeSH IDM0061939

Synonyms (39)

Synonym
AKOS001107057
benzotript
cr-501
SPECTRUM_001706
MLS000760874
smr000372176
benzotriptum [inn-latin]
einecs 254-500-0
benzotript [inn]
benzotripte [inn-french]
n-(p-chlorobenzoyl)-l-tryptophan
benzotripte
benzotripto [inn-spanish]
KBIO2_007322
KBIO2_002186
KBIO2_004754
KBIOSS_002186
(s)-2-(4-chloro-benzoylamino)-3-(1h-indol-3-yl)-propionic acid
bdbm50144035
CHEMBL63544 ,
39544-74-6
EN300-87510
(2s)-2-[(4-chlorobenzoyl)amino]-3-(1h-indol-3-yl)propanoic acid
NCGC00246028-01
HMS2736O06
unii-ls5o682bro
benzotripto
benzotriptum
ls5o682bro ,
2-(4-chloro-benzoylamino)-3-(1h-indol-3-yl)-propanoic acid
SCHEMBL93960
n-p-chlorobenzoyl-l-tryptophane
QJERBBQXOMUURJ-INIZCTEOSA-N
Z56821825
Q27283157
(4-chlorobenzoyl)-l-tryptophan
CS-0081358
DTXSID501043305
HY-121278

Research Excerpts

Dosage Studied

Proglumide and benzotript were able to inhibit the shift to the right of the dose-response curve for morphine. In the case of secretagogue stimulation, Benzotript slightly affected histamine-induced AP (15% inhibition at 5 X 10(-3) M), proglumide did not.

ExcerptRelevanceReference
" In the case of secretagogue stimulation (1) benzotript slightly affected histamine-induced AP (15% inhibition at 5 X 10(-3) M), proglumide did not; (2) both proglumide and benzotript inhibited in a non-competitive manner acetylcholine-induced AP; (3) these isolated cells were sensitive to gastrin and the dose-response curve for the stimulant was biphasic (maximum for 1 X 10(-9) M), suggesting a desensitization mechanism."( Evidence that proglumide and benzotript antagonize secretagogue stimulation of isolated gastric parietal cells.
Bali, JP; Magous, R, 1983
)
0.82
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency22.33420.140911.194039.8107AID2451
LuciferasePhotinus pyralis (common eastern firefly)Potency16.94410.007215.758889.3584AID588342
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
mitogen-activated protein kinase 1Homo sapiens (human)Potency6.30960.039816.784239.8107AID1454
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
gemininHomo sapiens (human)Potency17.28990.004611.374133.4983AID624296; AID624297
Glycoprotein hormones alpha chainHomo sapiens (human)Potency15.84894.46688.344810.0000AID624291
[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)
Integrin beta-2Homo sapiens (human)IC50 (µMol)169.00000.00080.59053.7800AID226860
Intercellular adhesion molecule 1Homo sapiens (human)IC50 (µMol)169.00000.00301.212210.0000AID226860
Integrin alpha-LHomo sapiens (human)IC50 (µMol)169.00000.00080.60203.7800AID226860
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50 (µMol)100.00000.00041.13803.5000AID52573
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (65)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell population proliferationGlycoprotein hormones alpha chainHomo sapiens (human)
hormone-mediated signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
regulation of signaling receptor activityGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of steroid biosynthetic processGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell migrationGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid gland developmentGlycoprotein hormones alpha chainHomo sapiens (human)
luteinizing hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid hormone generationGlycoprotein hormones alpha chainHomo sapiens (human)
microglial cell activationIntegrin beta-2Homo sapiens (human)
receptor-mediated endocytosisIntegrin beta-2Homo sapiens (human)
phagocytosis, engulfmentIntegrin beta-2Homo sapiens (human)
apoptotic processIntegrin beta-2Homo sapiens (human)
inflammatory responseIntegrin beta-2Homo sapiens (human)
cell adhesionIntegrin beta-2Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-matrix adhesionIntegrin beta-2Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-2Homo sapiens (human)
cell-cell signalingIntegrin beta-2Homo sapiens (human)
regulation of cell shapeIntegrin beta-2Homo sapiens (human)
neutrophil chemotaxisIntegrin beta-2Homo sapiens (human)
receptor internalizationIntegrin beta-2Homo sapiens (human)
positive regulation of superoxide anion generationIntegrin beta-2Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-2Homo sapiens (human)
endodermal cell differentiationIntegrin beta-2Homo sapiens (human)
receptor clusteringIntegrin beta-2Homo sapiens (human)
positive regulation of neutrophil degranulationIntegrin beta-2Homo sapiens (human)
negative regulation of dopamine metabolic processIntegrin beta-2Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationIntegrin beta-2Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusIntegrin beta-2Homo sapiens (human)
positive regulation of protein targeting to membraneIntegrin beta-2Homo sapiens (human)
amyloid-beta clearanceIntegrin beta-2Homo sapiens (human)
cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-cell adhesion via plasma-membrane adhesion moleculesIntegrin beta-2Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellIntegrin beta-2Homo sapiens (human)
neutrophil migrationIntegrin beta-2Homo sapiens (human)
positive regulation of prostaglandin-E synthase activityIntegrin beta-2Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-2Homo sapiens (human)
regulation of leukocyte mediated cytotoxicityIntercellular adhesion molecule 1Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntercellular adhesion molecule 1Homo sapiens (human)
T cell antigen processing and presentationIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of cellular extravasationIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte cell-cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
membrane to membrane dockingIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesion mediated by integrinIntercellular adhesion molecule 1Homo sapiens (human)
adhesion of symbiont to hostIntercellular adhesion molecule 1Homo sapiens (human)
symbiont entry into host cellIntercellular adhesion molecule 1Homo sapiens (human)
receptor-mediated virion attachment to host cellIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte migrationIntercellular adhesion molecule 1Homo sapiens (human)
establishment of endothelial barrierIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to glucose stimulusIntercellular adhesion molecule 1Homo sapiens (human)
T cell extravasationIntercellular adhesion molecule 1Homo sapiens (human)
regulation of ruffle assemblyIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to amyloid-betaIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to leukemia inhibitory factorIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntercellular adhesion molecule 1Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntegrin alpha-LHomo sapiens (human)
phagocytosisIntegrin alpha-LHomo sapiens (human)
inflammatory responseIntegrin alpha-LHomo sapiens (human)
cell adhesionIntegrin alpha-LHomo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntegrin alpha-LHomo sapiens (human)
leukocyte cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-LHomo sapiens (human)
signal transductionIntegrin alpha-LHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-LHomo sapiens (human)
memory T cell extravasationIntegrin alpha-LHomo sapiens (human)
receptor clusteringIntegrin alpha-LHomo sapiens (human)
cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-LHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
protein bindingGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
cargo receptor activityIntegrin beta-2Homo sapiens (human)
amyloid-beta bindingIntegrin beta-2Homo sapiens (human)
complement component C3b bindingIntegrin beta-2Homo sapiens (human)
integrin bindingIntegrin beta-2Homo sapiens (human)
protein bindingIntegrin beta-2Homo sapiens (human)
protein kinase bindingIntegrin beta-2Homo sapiens (human)
ICAM-3 receptor activityIntegrin beta-2Homo sapiens (human)
heat shock protein bindingIntegrin beta-2Homo sapiens (human)
metal ion bindingIntegrin beta-2Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-2Homo sapiens (human)
virus receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
transmembrane signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
integrin bindingIntercellular adhesion molecule 1Homo sapiens (human)
protein bindingIntercellular adhesion molecule 1Homo sapiens (human)
signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
protein bindingIntegrin alpha-LHomo sapiens (human)
ICAM-3 receptor activityIntegrin alpha-LHomo sapiens (human)
metal ion bindingIntegrin alpha-LHomo sapiens (human)
cell adhesion molecule bindingIntegrin alpha-LHomo sapiens (human)
integrin bindingIntegrin alpha-LHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
extracellular regionGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
Golgi lumenGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone complexGlycoprotein hormones alpha chainHomo sapiens (human)
pituitary gonadotropin complexGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
plasma membraneIntegrin beta-2Homo sapiens (human)
external side of plasma membraneIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
membraneIntegrin beta-2Homo sapiens (human)
integrin alphaL-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaM-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaX-beta2 complexIntegrin beta-2Homo sapiens (human)
specific granule membraneIntegrin beta-2Homo sapiens (human)
plasma membrane raftIntegrin beta-2Homo sapiens (human)
extracellular exosomeIntegrin beta-2Homo sapiens (human)
tertiary granule membraneIntegrin beta-2Homo sapiens (human)
ficolin-1-rich granule membraneIntegrin beta-2Homo sapiens (human)
extracellular vesicleIntegrin beta-2Homo sapiens (human)
integrin complexIntegrin beta-2Homo sapiens (human)
receptor complexIntegrin beta-2Homo sapiens (human)
focal adhesionIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
immunological synapseIntercellular adhesion molecule 1Homo sapiens (human)
extracellular spaceIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
focal adhesionIntercellular adhesion molecule 1Homo sapiens (human)
external side of plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
cell surfaceIntercellular adhesion molecule 1Homo sapiens (human)
membraneIntercellular adhesion molecule 1Homo sapiens (human)
membrane raftIntercellular adhesion molecule 1Homo sapiens (human)
collagen-containing extracellular matrixIntercellular adhesion molecule 1Homo sapiens (human)
extracellular exosomeIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntegrin alpha-LHomo sapiens (human)
cell surfaceIntegrin alpha-LHomo sapiens (human)
membraneIntegrin alpha-LHomo sapiens (human)
integrin alphaL-beta2 complexIntegrin alpha-LHomo sapiens (human)
specific granule membraneIntegrin alpha-LHomo sapiens (human)
extracellular exosomeIntegrin alpha-LHomo sapiens (human)
integrin complexIntegrin alpha-LHomo sapiens (human)
external side of plasma membraneIntegrin alpha-LHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID222271The compound was tested for the inhibition of CCK-8-stimulated amylase release; nd=No data1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
AID88496Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Structure-activity relationships of C-terminal tri- and tetrapeptide fragments that inhibit gastrin activity.
AID177912Inhibition of gastrin stimulated acid secretion in in situ perfused rat stomach1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Structure-activity relationships of C-terminal tri- and tetrapeptide fragments that inhibit gastrin activity.
AID52573Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
AID50835The compound was tested for the inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type B receptor in guinea pig cerebral cortical; nd=No data1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
AID226860Inhibitory activity against association of LFA-1 with intercellular adhesion molecule 12004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-199016 (42.11)18.7374
1990's11 (28.95)18.2507
2000's6 (15.79)29.6817
2010's4 (10.53)24.3611
2020's1 (2.63)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.43

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 Index10.43 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index4.12 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.43)

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%
Other39 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]