Page last updated: 2024-12-11

gr 94800

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

Description

GR 94800: a selective NK2 heptapeptide antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5487475
CHEMBL ID2370064
SCHEMBL ID16353709
MeSH IDM0233626

Synonyms (19)

Synonym
chembl2370064 ,
bdbm50048413
l-norleucinamide, n-benzoyl-l-alanyl-l-alanyl-d-tryptophyl-l-phenylalanyl-d-prolyl-l-prolyl-
gr-94800
n-alpha-benzoylalanyl-alanyl-tryptophyl-phenylalanyl-prolyl-prolyl-norleucinamide
gr 94800
nalpha-benzoyl-ala-ala-d-trp-phe-d-pro-pro-nle-nh2
(2s)-n-[(2s)-1-amino-1-oxohexan-2-yl]-1-[(2r)-1-[(2s)-2-[[(2r)-2-[[(2s)-2-[[(2s)-2-benzamidopropanoyl]amino]propanoyl]amino]-3-(1h-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide
n-alpha-benzoyl-ala-ala-d-trp-phe-d-pro-pro-nle-nh2
141636-65-9
AKOS024456735
DTXSID00161781
l-norleucinamide,n-benzoyl-l-alanyl-l-alanyl-d-tryptophyl-l-phenylalanyl-d-prolyl-l-prolyl-
SCHEMBL16353709
gr 94800, >96%, powder
phco-ala-ala-d-trp-phe-d-pro-pro-nle-nh2
bz-ala-ala-d-trp-phe-d-pro-pro-nle-nh(2)
(s)-n-((s)-1-amino-1-oxohexan-2-yl)-1-(benzoyl-l-alanyl-l-alanyl-d-tryptophyl-l-phenylalanyl-d-prolyl)pyrrolidine-2-carboxamide
PD071165
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-K receptorHomo sapiens (human)Ki0.00020.00011.92429.7930AID1181861
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1181861Displacement of [3H]GR100679 from NK2 receptor (unknown origin) expressed in CHO/T cells2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Toward fluorescent probes for G-protein-coupled receptors (GPCRs).
AID212392Compound was evaluated for antagonism of contractile response of rat portal vein at Tachykinin receptor 31992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
AID208251Compound was evaluated for antagonism of contractile response of guinea pig ileum longitudinal smooth muscle (GPI) at Tachykinin receptor 11992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
AID212058Compound was evaluated for antagonism of contractile response of rat colon muscularis mucosae (RC) at Tachykinin receptor 21992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (76.92)18.2507
2000's1 (7.69)29.6817
2010's2 (15.38)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: 11.68

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 Index11.68 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (92.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]