Page last updated: 2024-12-10

sr 142948

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

Description

SR 142948: structurally similar to SR-48692 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311451
CHEMBL ID3040381
CHEMBL ID2431105
CHEBI ID93589
SCHEMBL ID7558783
MeSH IDM0296199

Synonyms (44)

Synonym
HMS3268L04
BRD-K91243525-001-01-5
gtpl1580
2-[[5-(2,6-dimethoxyphenyl)-1-[4-(3-dimethylaminopropyl-methylcarbamoyl)-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid
PDSP1_001736
PDSP2_001719
sr142948a
NCGC00167732-01
L015605
2-[[5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid
sr-142948a
MLS-0437457.0001
SCHEMBL7558783
cas_184162-64-9
bdbm85050
184162-64-9
sr 142948
sr-142948
CHEMBL3040381
chembl2431105 ,
bdbm50440738
2-[5-(2,6-dimethoxyphenyl)-1-[4-[n-methyl-n-(3-dimethylaminopropyl)carbamoyl]-2-isopropylphenyl]-3-pyrazolylcarbonylamino]-2-adamantanecarboxylic acid
LWULHXVBLMWCHO-UHFFFAOYSA-N
2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1h-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
2-[(5-(2,6-dimethoxy-phenyl)-1-{4-[(3-dimethylamino-propyl)-methyl-carbamoyl]-2-isopropyl-phenyl}-1h-pyrazole-3-carbonyl)-amino]-adamantane-2-carboxylic acid
DTXSID50415529
2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1h-pyrazol-3-yl]carbonyl]amino]tricyclo[3.3.1.13,7]decane-2-carboxylic acid
AKOS024457043
184162-21-8
CHEBI:93589
HY-107664
J-011801
184162-64-9 (free base)
Q7392758
NCGC00167732-04
HMS3740A03
q6n ,
2-[[5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methyl-carbamoyl]-2-propan-2-yl-phenyl]pyrazol-3-yl]carbonylamino]adamantane-2-carboxylic acid
tricyclo(3.3.1.13,7)decane-2-carboxylic acid, 2-(((5-(2,6-dimethoxyphenyl)-1-(4-(((3-(dimethylamino)propyl)methylamino)carbonyl)-2-(1-methylethyl)phenyl)-1h-pyrazol-3-yl)carbonyl)amino)-
sr142948
2-(((5-(2,6-dimethoxyphenyl)-1-(4-(((3-(dimethylamino)propyl)methylamino)carbonyl)-2-(1-methylethyl)phenyl)-1h-pyrazol-3-yl)carbonyl)amino)tricyclo(3.3.1.13,7)decane-2-carboxylic acid
w59c8b2mzs ,
CS-0029137
E98719

Research Excerpts

Overview

SR 142948 is an original and extremely potent neurotensin receptor antagonist developed in a promising approach to novel antipsychotic drugs.

ExcerptReferenceRelevance
"SR 142948 is an original and extremely potent neurotensin receptor antagonist developed in a promising approach to novel antipsychotic drugs. "( X-ray structural characterization of SR 142948, a novel potent synthetic neurotensin receptor antagonist.
Boigegrain, R; Durant, F; Gully, D; Labeeuw, B; Longfils, G; Quéré, L, 1998
)
2.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-acyl-amino acidA carboxamide resulting from the formal condensation of a carboxylic acid with the amino group of an amino acid.
[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 (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency89.12510.003245.467312,589.2998AID2517
[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)
Neurotensin receptor type 2Homo sapiens (human)Ki0.07400.00050.04710.4180AID1055239
Neurotensin receptor type 1Rattus norvegicus (Norway rat)Ki0.00170.00110.00180.0026AID1161615; AID1176214
Neurotensin receptor type 1Homo sapiens (human)IC50 (µMol)0.00370.00020.00730.0820AID1182265; AID1289937; AID1577246
Neurotensin receptor type 1Homo sapiens (human)Ki0.00110.00010.00100.0033AID1055241; AID1289937
Neurotensin receptor type 2Rattus norvegicus (Norway rat)Ki0.00630.00580.09170.6440AID1154142; AID1161616; AID1176215
[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 1Homo sapiens (human)EC50 (µMol)56.50002.710010.320019.6000AID602356; AID602427
Neurotensin receptor type 1Homo sapiens (human)Kd0.00040.00040.01300.0330AID1802507
Neurotensin receptor type 2Rattus norvegicus (Norway rat)EC50 (µMol)0.02000.01800.07080.2170AID1154139; AID1161613; AID1176211
[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)Ke0.00150.00150.01310.0230AID1154138
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
sensory perceptionNeurotensin receptor type 2Homo sapiens (human)
regulation of membrane potentialNeurotensin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
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 2Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 2Homo sapiens (human)
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
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
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 (20)

Assay IDTitleYearJournalArticle
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.
AID1176214Displacement of [125L]NT from rat neurotensin receptor type 1 expressed in CHOK1 cells by radioligand binding assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
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.
AID1289937Displacement of [3H]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29 cells after 2 hrs by liquid scintillation counting2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1577246Antagonist activity at NTR1 (unknown origin)2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
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.
AID1176215Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID1055239Displacement of [3H]NT(8 to 13) from human NTS2 receptor expressed in HEK293 cells2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
AID1289949Displacement of [3H]NT(8 to 13 residues) from human NTSR2 expressed in HEK293 cell membranes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1161616Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID1055241Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
AID1161613Agonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as calcium mobilization by FLIPR assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID1176211Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID1182265Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
AID1161615Displacement of [125I]neurotensin from rat NTS1 receptor expressed in CHO-K1 cells by competitive binding assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for 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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346344Human NTS1 receptor (Neurotensin receptors)1997The Journal of pharmacology and experimental therapeutics, Feb, Volume: 280, Issue:2
Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
AID1802507SPR Screening Assay from Article 10.1021/acschembio.6b00646: \\Ligand Discovery for a Peptide-Binding GPCR by Structure-Based Screening of Fragment- and Lead-Like Chemical Libraries.\\2017ACS chemical biology, 03-17, Volume: 12, Issue:3
Ligand Discovery for a Peptide-Binding GPCR by Structure-Based Screening of Fragment- and Lead-Like Chemical Libraries.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (16.13)18.2507
2000's8 (25.81)29.6817
2010's16 (51.61)24.3611
2020's2 (6.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.39

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 Index11.39 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.85 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.39)

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%
Other31 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]