Page last updated: 2024-11-13

knt 127

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

Cross-References

ID SourceID
PubMed CID52942137
CHEMBL ID1270282
MeSH IDM0553859

Synonyms (8)

Synonym
bdbm50329095
CHEMBL1270282 ,
knt-127
1256921-89-7
CS-0078209
HY-120511
AKOS040746962
EX-A7846F
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ki0.00020.00000.53939.4000AID526327; AID689648
Mu-type opioid receptorMus musculus (house mouse)Ki0.02130.00000.12281.3000AID526326; AID689647
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID526332Analgesic activity in subcutaneously dosed mouse assessed as inhibition of acetic-acid-induced writhings2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID1877607Increase in number of nociceptive behaviors in mouse at 3 to 30 ug, it2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID689650Selectivity ratio of Ki for mu opioid receptor in mouse whole brain without cerebellum to Ki for delta opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
AID1461556Antimicrobial activity against Trichomonas vaginalis after 48 hrs by neutral red staining based invert microscopic analysis2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
AID526328Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum membranes2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID1877609Increase in number of nociceptive behaviors in mouse at 30 ug, it2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID1877604Agonist activity at MRGPRX2 (unknown origin) expressed in HEK293 cells assessed as induction of G(o) dissociation by measuring luminescent decay at 32 uM by NanoBiT-G-protein dissociation assay2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID526329Selectivity ratio, ratio of Ki for mouse brain mu opioid receptor to Ki for mouse brain delta opioid receptor2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID689648Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
AID526327Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID1877610Increase in number of scratching behaviors in mouse at 3 to 300 ug, id2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID526326Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID689651Selectivity ratio of Ki for kappa opioid receptor in guinea pig cerebellum to Ki for delta opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
AID1668244Antidepressant activity in mouse at 10 mg/kg, sc by forced swim tes2020Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
AID1668241Antidepressant activity in sc dosed mouse assessed as increase in total swimming count by forced swim test2020Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
AID526330Selectivity ratio, ratio of Ki for mouse brain mu opioid receptor to Ki for guinea pig cerebellum kappa opioid receptor2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
AID1668240Antidepressant activity in sc dosed mouse assessed as decrease in total immobility count by forced swim test2020Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
AID1877606Agonist activity at mouse Mrgprb2 expressed in HEK293 cells assessed as induction of G(o) dissociation by measuring luminescent decay at 32 uM by NanoBiT-G-protein dissociation assay2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID689647Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
AID1877611Increase in number of scratching behaviors in mouse at 400 ug, id trated after dosing of subcutaneous dosing of antipruritic-nalfurafin2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID1877602Binding affinity to opioid receptor (unknown origin)2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID1668242Antidepressant activity in sc dosed mouse assessed as increase in climbing count by forced swim test2020Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
AID1877608Increase in number of nociceptive behaviors in mouse at 30 ug, it treated 5 mins after intrathecal dose of MRGPRX2/Mrgprb2 antagonist QWF2022Bioorganic & medicinal chemistry letters, 01-15, Volume: 56Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands.
AID689649Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (60.00)24.3611
2020's2 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.87

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.87 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.87)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]