Page last updated: 2024-11-12

sr 48527

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

Description

SR 48527: SR 48527 is the S-enantiomer; SR-49711 is the R-enantiomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9915499
CHEMBL ID461604
SCHEMBL ID18983298
MeSH IDM0229284

Synonyms (13)

Synonym
gtpl1581
(2s)-2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]-2-cyclohexylacetic acid
sr48527
CHEMBL461604 ,
sr-48527
sr 48527
bdbm82417
SCHEMBL18983298
Q27088865
cid 9915499
156579-04-3
cyclohexaneacetic acid, alpha-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1h-pyrazol-3-yl]carbonyl]amino]-, (alphas)-
AKOS040749557
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Rattus norvegicus (Norway rat)Ki0.64400.00580.09170.6440AID1154142
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Rattus norvegicus (Norway rat)EC50 (µMol)0.21700.01800.07080.2170AID1154139
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 1Rattus norvegicus (Norway rat)Ke0.02300.00150.01310.0230AID1154138; AID1195278
Neurotensin receptor type 1Homo sapiens (human)Ke0.03500.03500.03550.0360AID418188
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
positive regulation of gene expressionNeurotensin receptor type 1Homo sapiens (human)
temperature homeostasisNeurotensin receptor type 1Homo sapiens (human)
negative regulation of systemic arterial blood pressureNeurotensin receptor type 1Homo sapiens (human)
regulation of membrane depolarizationNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
chemical synaptic transmissionNeurotensin receptor type 1Homo sapiens (human)
learningNeurotensin receptor type 1Homo sapiens (human)
adult locomotory behaviorNeurotensin receptor type 1Homo sapiens (human)
positive regulation of glutamate secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionNeurotensin receptor type 1Homo sapiens (human)
response to lipidNeurotensin receptor type 1Homo sapiens (human)
positive regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
negative regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
regulation of respiratory gaseous exchangeNeurotensin receptor type 1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painNeurotensin receptor type 1Homo sapiens (human)
negative regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inositol phosphate biosynthetic processNeurotensin receptor type 1Homo sapiens (human)
D-aspartate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
inositol phosphate catabolic processNeurotensin receptor type 1Homo sapiens (human)
positive regulation of arachidonic acid secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inhibitory postsynaptic potentialNeurotensin receptor type 1Homo sapiens (human)
L-glutamate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityNeurotensin receptor type 1Homo sapiens (human)
protein bindingNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 1Homo sapiens (human)
identical protein bindingNeurotensin receptor type 1Homo sapiens (human)
protein-containing complex bindingNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
endoplasmic reticulumNeurotensin receptor type 1Homo sapiens (human)
Golgi apparatusNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cell surfaceNeurotensin receptor type 1Homo sapiens (human)
symmetric synapseNeurotensin receptor type 1Homo sapiens (human)
terminal boutonNeurotensin receptor type 1Homo sapiens (human)
dendritic spineNeurotensin receptor type 1Homo sapiens (human)
dendritic shaftNeurotensin receptor type 1Homo sapiens (human)
perikaryonNeurotensin receptor type 1Homo sapiens (human)
membrane raftNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID418188Apparent affinity to NTR1 receptor expressed in CHOK1 cells2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
AID418185Agonist activity at NTR1 expressed in CHOK1 cells assessed as stimulation of calcium mobilization at 10 uM relative to neurotensin2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
AID1195278Antagonist activity at rat NTS1 overexpressed in CHO-k1 cells assessed as blockade of neurotensin-mediated calcium mobilization after 15 mins by FLIPR assay2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.
AID1154139Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1154140Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay relative to SR142948a2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1154142Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1154138Antagonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as inhibition of NT-induced calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1195276Displacement of [I125]neurotensin from rat NTS1 overexpressed in CHO-k1 cells by competitive binding Assay2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.
AID1346391Rat NTS1 receptor (Neurotensin receptors)1995Molecular pharmacology, May, Volume: 47, Issue:5
[3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (75.00)18.2507
2000's1 (8.33)29.6817
2010's2 (16.67)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: 12.04

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 Index12.04 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]