Page last updated: 2024-11-12

l 054522

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

Description

L 054522: somatostatin receptor subtype 2 agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15965425
CHEMBL ID99895
MeSH IDM0295097

Synonyms (23)

Synonym
l054522
l 054522
gtpl2046
tert-butyl (2s)-6-amino-2-[[(2r,3s)-3-(1h-indol-3-yl)-2-[[4-(2-oxo-3h-benzimidazol-1-yl)piperidine-1-carbonyl]amino]butanoyl]amino]hexanoate
CHEMBL99895 ,
6-amino-2-(3-(1h-indol-3-yl)-2-{[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidine-1-carbonyl]-amino}-butyrylamino)-hexanoic acid tert-butyl ester
bdbm50103430
l-054,522
l-054522
tert-butyl (2s)-6-amino-2-(((2r,3s)-3-(1h-indol-3-yl)-2-((4-(2-oxo-3h-benzimidazol-1-yl)piperidine-1-carbonyl)amino)butanoyl)amino)hexanoate
7w8x3axg75 ,
n-(4-(2-oxo-2,3-dihydro-1h-benzimidazol-1-yl)piperidin-1-ylcarbonyl)-(3(s)-methyl)-d-tryptophyl-l-lysine tert-butyl ester
(betas)-n-((4-(2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)carbonyl)-beta-methyl-d-tryptophyl-l-lysine 1,1-dimethylethyl ester
unii-7w8x3axg75
l-lysine, (betas)-n-((4-(2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)carbonyl)-beta-methyl-d-tryptophyl-, 1,1-dimethylethyl ester
cid 15965425
214348-67-1
GI9 ,
tert-butyl (2s)-6-azanyl-2-[[(2r,3s)-3-(1h-indol-3-yl)-2-[[4-(2-oxidanylidene-3h-benzimidazol-1-yl)piperidin-1-yl]carbonylamino]butanoyl]amino]hexanoate
l-054,52
(.beta.s)-n-((4-(2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)carbonyl)-.beta.-methyl-d-tryptophyl-l-lysine 1,1-dimethylethyl ester
l-lysine, (.beta.s)-n-((4-(2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)carbonyl)-.beta.-methyl-d-tryptophyl-, 1,1-dimethylethyl ester
AKOS040748694

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Backbone cyclization of urea-based somatostatin agonists resulted in novel, orally bioavailable agonists."( Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
Birzin, ET; Cheng, K; Huskey, SE; Jacks, T; Marino, D; Mosley, R; Pan, Y; Pasternak, A; Patchett, AA; Rohrer, SP; Sanderson, PE; Schaeffer, JM; Schleim, KD; Yang, L, 1999
)
0.3

Dosage Studied

ExcerptRelevanceReference
"8 nM (where K(B) is the concentration of antagonist that shifts the agonist dose-response 2-fold)."( Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
Bigg, D; Contour-Galcéra, MO; Lannoy, J; Moinet, C; Plas, P; Poitout, L; Pommier, J; Roubert, P; Thurieau, C, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Somatostatin receptor type 1Homo sapiens (human)Ki2.39200.00030.41232.3920AID203262
Somatostatin receptor type 2Homo sapiens (human)Ki0.00000.00000.40914.7200AID203400; AID203405
Somatostatin receptor type 4Homo sapiens (human)Ki0.08100.00060.27333.2000AID203563
Somatostatin receptor type 3Homo sapiens (human)Ki0.03100.00010.03200.1290AID203420
Somatostatin receptor type 5Homo sapiens (human)Ki0.16300.00010.44794.0700AID203581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (23)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerSomatostatin receptor type 1Homo sapiens (human)
glutamate receptor signaling pathwaySomatostatin receptor type 1Homo sapiens (human)
spermatogenesisSomatostatin receptor type 1Homo sapiens (human)
negative regulation of cell population proliferationSomatostatin receptor type 1Homo sapiens (human)
cerebellum developmentSomatostatin receptor type 1Homo sapiens (human)
forebrain developmentSomatostatin receptor type 1Homo sapiens (human)
somatostatin signaling pathwaySomatostatin receptor type 1Homo sapiens (human)
response to starvationSomatostatin receptor type 1Homo sapiens (human)
cellular response to leukemia inhibitory factorSomatostatin receptor type 1Homo sapiens (human)
cellular response to estradiol stimulusSomatostatin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwaySomatostatin receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerSomatostatin receptor type 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySomatostatin receptor type 2Homo sapiens (human)
spermatogenesisSomatostatin receptor type 2Homo sapiens (human)
negative regulation of cell population proliferationSomatostatin receptor type 2Homo sapiens (human)
cerebellum developmentSomatostatin receptor type 2Homo sapiens (human)
peristalsisSomatostatin receptor type 2Homo sapiens (human)
forebrain developmentSomatostatin receptor type 2Homo sapiens (human)
somatostatin signaling pathwaySomatostatin receptor type 2Homo sapiens (human)
response to starvationSomatostatin receptor type 2Homo sapiens (human)
cellular response to glucocorticoid stimulusSomatostatin receptor type 2Homo sapiens (human)
cellular response to estradiol stimulusSomatostatin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwaySomatostatin receptor type 2Homo sapiens (human)
G protein-coupled receptor signaling pathwaySomatostatin receptor type 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerSomatostatin receptor type 4Homo sapiens (human)
negative regulation of cell population proliferationSomatostatin receptor type 4Homo sapiens (human)
cell migrationSomatostatin receptor type 4Homo sapiens (human)
forebrain developmentSomatostatin receptor type 4Homo sapiens (human)
somatostatin signaling pathwaySomatostatin receptor type 4Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeSomatostatin receptor type 4Homo sapiens (human)
positive regulation of arachidonic acid secretionSomatostatin receptor type 4Homo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaySomatostatin receptor type 4Homo sapiens (human)
neuropeptide signaling pathwaySomatostatin receptor type 4Homo sapiens (human)
cellular response to glucocorticoid stimulusSomatostatin receptor type 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerSomatostatin receptor type 3Homo sapiens (human)
cell-cell signalingSomatostatin receptor type 3Homo sapiens (human)
spermatogenesisSomatostatin receptor type 3Homo sapiens (human)
negative regulation of cell population proliferationSomatostatin receptor type 3Homo sapiens (human)
hormone-mediated apoptotic signaling pathwaySomatostatin receptor type 3Homo sapiens (human)
cerebellum developmentSomatostatin receptor type 3Homo sapiens (human)
forebrain developmentSomatostatin receptor type 3Homo sapiens (human)
somatostatin signaling pathwaySomatostatin receptor type 3Homo sapiens (human)
response to starvationSomatostatin receptor type 3Homo sapiens (human)
cellular response to glucocorticoid stimulusSomatostatin receptor type 3Homo sapiens (human)
cellular response to estradiol stimulusSomatostatin receptor type 3Homo sapiens (human)
neuropeptide signaling pathwaySomatostatin receptor type 3Homo sapiens (human)
G protein-coupled receptor signaling pathwaySomatostatin receptor type 5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerSomatostatin receptor type 5Homo sapiens (human)
negative regulation of cell population proliferationSomatostatin receptor type 5Homo sapiens (human)
positive regulation of cytokinesisSomatostatin receptor type 5Homo sapiens (human)
somatostatin signaling pathwaySomatostatin receptor type 5Homo sapiens (human)
cellular response to glucocorticoid stimulusSomatostatin receptor type 5Homo sapiens (human)
neuropeptide signaling pathwaySomatostatin receptor type 5Homo sapiens (human)
regulation of insulin secretionSomatostatin receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
somatostatin receptor activitySomatostatin receptor type 1Homo sapiens (human)
protein bindingSomatostatin receptor type 1Homo sapiens (human)
neuropeptide bindingSomatostatin receptor type 1Homo sapiens (human)
protein bindingSomatostatin receptor type 2Homo sapiens (human)
PDZ domain bindingSomatostatin receptor type 2Homo sapiens (human)
somatostatin receptor activitySomatostatin receptor type 2Homo sapiens (human)
neuropeptide bindingSomatostatin receptor type 2Homo sapiens (human)
protein bindingSomatostatin receptor type 4Homo sapiens (human)
somatostatin receptor activitySomatostatin receptor type 4Homo sapiens (human)
neuropeptide bindingSomatostatin receptor type 4Homo sapiens (human)
somatostatin receptor activitySomatostatin receptor type 3Homo sapiens (human)
signaling receptor bindingSomatostatin receptor type 3Homo sapiens (human)
protein bindingSomatostatin receptor type 3Homo sapiens (human)
neuropeptide bindingSomatostatin receptor type 3Homo sapiens (human)
G protein-coupled receptor activitySomatostatin receptor type 3Homo sapiens (human)
protein bindingSomatostatin receptor type 5Homo sapiens (human)
neuropeptide bindingSomatostatin receptor type 5Homo sapiens (human)
somatostatin receptor activitySomatostatin receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membraneSomatostatin receptor type 1Homo sapiens (human)
plasma membraneSomatostatin receptor type 1Homo sapiens (human)
neuron projectionSomatostatin receptor type 1Homo sapiens (human)
cytosolSomatostatin receptor type 2Homo sapiens (human)
plasma membraneSomatostatin receptor type 2Homo sapiens (human)
neuron projectionSomatostatin receptor type 2Homo sapiens (human)
plasma membraneSomatostatin receptor type 2Homo sapiens (human)
plasma membraneSomatostatin receptor type 4Homo sapiens (human)
neuron projectionSomatostatin receptor type 4Homo sapiens (human)
plasma membraneSomatostatin receptor type 4Homo sapiens (human)
plasma membraneSomatostatin receptor type 3Homo sapiens (human)
ciliumSomatostatin receptor type 3Homo sapiens (human)
ciliary membraneSomatostatin receptor type 3Homo sapiens (human)
non-motile ciliumSomatostatin receptor type 3Homo sapiens (human)
neuron projectionSomatostatin receptor type 3Homo sapiens (human)
plasma membraneSomatostatin receptor type 3Homo sapiens (human)
plasma membraneSomatostatin receptor type 5Homo sapiens (human)
plasma membraneSomatostatin receptor type 5Homo sapiens (human)
neuron projectionSomatostatin receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID203400Binding affinity towards Somatostatin receptor type 2 (hsst2)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID203563Binding affinity towards Somatostatin receptor type 4 (hsst4)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID203420Binding affinity towards Somatostatin receptor type 3 (hsst3)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID203262Binding affinity towards Somatostatin receptor type 1 (hsst1)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID203405Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypes2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
AID203581Binding affinity towards Somatostatin receptor type 5 (hsst5)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID1346424Human SST2 receptor (Somatostatin receptors)1998Proceedings of the National Academy of Sciences of the United States of America, Sep-01, Volume: 95, Issue:18
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (33.33)18.2507
2000's4 (66.67)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.46

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.46 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (14.29%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]