Page last updated: 2024-11-12

sr 14150

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

Description

SR 14150: mixed NOP and mu-opioid receptor ligand and antinociceptive; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9905428
CHEMBL ID101454
SCHEMBL ID15794608
MeSH IDM0521523

Synonyms (15)

Synonym
bdbm50147740
1-(1-cyclooctyl-piperidin-4-yl)-1,3-dihydro-indol-2-one
CHEMBL101454 ,
709024-69-1
2h-indol-2-one, 1-(1-cyclooctyl-4-piperidinyl)-1,3-dihydro-
SCHEMBL15794608
1-(1-cyclooctylpiperidin-4-yl)-3h-indol-2-one
DTXSID60432666
sr-14150
sr14150
1-(1-cyclooctylpiperidin-4-yl)-indolin-2-one
unii-1o88c1nas7
sr 14150
1o88c1nas7 ,
AKOS040746374
[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)
Mu-type opioid receptorHomo sapiens (human)Ki0.02990.00000.419710.0000AID150850; AID1628144; AID749840
Kappa-type opioid receptorHomo sapiens (human)Ki0.04270.00000.362410.0000AID147995; AID749839
Nociceptin receptorHomo sapiens (human)Ki0.00140.00000.03370.5000AID1282209; AID147410; AID1628143; AID749841
[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)
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.09900.00000.32639.4000AID749836
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.27600.00000.22448.9900AID749834
Nociceptin receptorHomo sapiens (human)EC50 (µMol)0.02060.00010.00890.0630AID147409; AID1628145; AID749838
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (48)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
calcium-mediated signalingNociceptin receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
sensory perceptionNociceptin receptorHomo sapiens (human)
sensory perception of painNociceptin receptorHomo sapiens (human)
response to estradiolNociceptin receptorHomo sapiens (human)
positive regulation of urine volumeNociceptin receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayNociceptin receptorHomo sapiens (human)
eating behaviorNociceptin receptorHomo sapiens (human)
negative regulation of cAMP-mediated signalingNociceptin receptorHomo sapiens (human)
estrous cycleNociceptin receptorHomo sapiens (human)
negative regulation of blood pressureNociceptin receptorHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
regulation of locomotor rhythmNociceptin receptorHomo sapiens (human)
conditioned place preferenceNociceptin receptorHomo sapiens (human)
neuropeptide signaling pathwayNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
nociceptin receptor activityNociceptin receptorHomo sapiens (human)
G protein-coupled receptor activityNociceptin receptorHomo sapiens (human)
protein bindingNociceptin receptorHomo sapiens (human)
neuropeptide bindingNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneNociceptin receptorHomo sapiens (human)
cytoplasmic vesicleNociceptin receptorHomo sapiens (human)
plasma membraneNociceptin receptorHomo sapiens (human)
neuron projectionNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID150850Binding affinity against human Opioid receptor mu 1 on CHO cell membranes was determined by [3H]DAMGO displacement.2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID1628144Displacement of [3H]DAMGO from recombinant human mu opioid receptor expressed in CHO cell membranes2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
AID749839Displacement of [3H] U69593 from human kappa opioid receptor transfected in CHO cells2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID749841Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID749838Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID147995Binding affinity against human Opioid receptor kappa 1 on CHO cell membranes by [3H]U-69593 displacement.2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID147410Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID749835Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID147412Percent stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID749840Displacement of [3H]DAMGO from human mu opioid receptor transfected in CHO cells2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID147409Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID148370Inhibition of [3H]Cl-DPDPE binding to human opioid receptor delta 1 expressed in CHO cells; Not determined2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
AID1628145Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
AID1628143Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
AID749833Agonist activity at human kappa opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID749834Agonist activity at human kappa opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID749837Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID749836Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
AID1282209Displacement of [3H]N/OFQ from human nociceptin receptor2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
[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's0 (0.00)18.2507
2000's2 (33.33)29.6817
2010's4 (66.67)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: 12.79

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 Index12.79 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]