Compounds > tak-683
Page last updated: 2024-11-13

tak-683

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

Description

TAK-683: has antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID49787129
CHEMBL ID3314224
SCHEMBL ID12624944
MeSH IDM0581159

Synonyms (7)

Synonym
CHEMBL3314224 ,
SCHEMBL12624944
tak-683
bdbm50045507
CS-0109310
HY-P2161
AKOS040764212

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events were similar between TAK-683 and placebo subjects at all dose levels."( Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men.
Ahmad, I; Howard, K; MacLean, D; Oliva, C; Scott, G; Warrington, S; Wilbraham, D; Worthington, P, 2013)		0.87

Dosage Studied

ExcerptRelevanceReference
" Luteinizing hormone and follicle stimulating hormone concentrations were suppressed with TAK-683 continuous dosing compared with placebo by up to 70 and 43%, respectively, but this was not consistently dose-dependent."( Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men.
Ahmad, I; Howard, K; MacLean, D; Oliva, C; Scott, G; Warrington, S; Wilbraham, D; Worthington, P, 2013)		0.82
" This profound testosterone-lowering effect was sustained throughout 4-week dosing periods."( Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.
Akinaga, Y; Ban, J; Ikeda, Y; Kiba, A; Kumano, S; Kusaka, M; Masaki, T; Matsui, H; Matsumoto, S; Nakata, D; Ohtaki, T; Suzuki, A; Takatsu, Y; Tanaka, A; Watanabe, T; Yamaguchi, M, 2014)		0.63
[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)
KiSS-1 receptorRattus norvegicus (Norway rat)Ki0.00010.00010.00010.0001AID1179682
KiSS-1 receptorHomo sapiens (human)Ki0.00000.00000.60023.6000AID1179681
[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)
KiSS-1 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00130.00130.00270.0042AID1179679; AID1321526
KiSS-1 receptorHomo sapiens (human)EC50 (µMol)0.00030.00000.00230.0173AID1179678; AID1321525
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (2)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayKiSS-1 receptorHomo sapiens (human)
neuropeptide signaling pathwayKiSS-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
protein bindingKiSS-1 receptorHomo sapiens (human)
neuropeptide receptor activityKiSS-1 receptorHomo sapiens (human)
G protein-coupled peptide receptor activityKiSS-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneKiSS-1 receptorHomo sapiens (human)
ciliumKiSS-1 receptorHomo sapiens (human)
cell surfaceKiSS-1 receptorHomo sapiens (human)
membraneKiSS-1 receptorHomo sapiens (human)
intracellular membrane-bounded organelleKiSS-1 receptorHomo sapiens (human)
plasma membraneKiSS-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (54)

Assay IDTitleYearJournalArticle
AID1179689Stability of the compound in aqueous solution assessed as residual ratio at pH 7 up to 1 week by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179688Stability of the compound in aqueous solution assessed as residual ratio at pH 5 up to 1 week by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321540Volume of distribution in steady state in Sprague-Dawley rat plasma at 1 mg/kg, iv up to 24 hrs by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321538Plasma concentration in Sprague-Dawley rat at 1 mg/kg, iv after 5 mins by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321545MRT in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179693Stability of the compound in aqueous solution assessed as residual ratio at pH 7 up to 2 weeks by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179708Stimulation of LH release in Crl:CD(SD) rat assessed as LH AUC (0 to 4 hrs) at 0.01 to 1 nmol/kg, sc single dose relative to metastin2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179706Bioavailability in Sprague-Dawley rat at 1 mg/kg, sc after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179702Cmax in Sprague-Dawley rat at 1 mg/kg, sc after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179697Cmin in Sprague-Dawley rat at 1 mg/kg, iv after 5 mins by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321549Conformational changes of the compound in distilled water assessed as decrease in beta-sheet content at 0.1 mg/ml by preliminary circular dichroism analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179692Stability of the compound in aqueous solution assessed as residual ratio at pH 5 up to 2 weeks by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179694Testosterone-suppressive activity in Crl:CD(SD) rat assessed as number of animal with plasma testosterone level below the limit of detection at 0.05 mol/hr, sc through osmotic pumps measured after 6 days by RIA2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321550MRT in Sprague-Dawley rat plasma at 1 mg/kg, iv by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321548Inhibition of testosterone levels in sc dosed Crl:CD(SD) rat plasma assessed as compound dosing causing plasma testosterone level <0.04 ng/ml in all tested animals administered as continuous dosing through alzet osmotic pump for 1 to 4 weeks by radio-immu2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179686Stability of the compound in aqueous solution (JP1) assessed as residual ratio at pH 1.2 up to 1 week by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321546Bioavailability in Sprague-Dawley rat plasma at 1 mg/kg, sc up to 24 hrs by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321543Tmax in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321529Inhibition of testosterone levels in CD(SD) rat assessed as plasma testosterone level <0.04 ng/ml at 0.01 nmol/hr, sc administered continuously for 6 days through alzet osmotic pump measured after 6 days by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179687Stability of the compound in aqueous solution assessed as residual ratio at pH 3 up to 1 week by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179700Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321544AUC (0 to 24 hrs) in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179704AUC (0 to 24 hrs) in Sprague-Dawley rat at 1 mg/kg, sc after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179679Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321532Inhibition of testosterone levels in Crl:CD(SD) rat plasma assessed as plasma testosterone level <0.04 ng/ml at 3 pmol/hr, sc administered as continuous dosing through alzet osmotic pump for 4 weeks by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179695Testosterone-suppressive activity in Crl:CD(SD) rat assessed as number of animal with plasma testosterone level below the limit of detection at 0.03 mol/hr, sc through osmotic pumps measured after 6 days by RIA2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179678Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179703Tmax in Sprague-Dawley rat at 1 mg/kg, sc after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321534Inhibition of testosterone levels in Crl:CD(SD) rat plasma assessed as plasma testosterone level <0.04 ng/ml at 30 pmol/hr, sc administered as continuous dosing through alzet osmotic pump for 1 week by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321525Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179681Displacement of radioligand from human KISS1R transfected in CHO cells2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179685Testosterone-suppressive activity in Crl:CD(SD) rat assessed as number of animal with plasma testosterone level below the limit of detection at 0.1 nmol/hr, sc through osmotic pumps measured after 6 days by RIA2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179682Displacement of radioligand from rat KISS1R transfected in CHO cells2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179711Toxicity in dog2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179707Testosterone-suppressive activity in Crl:CD(SD) rat assessed as plasma testosterone level below the limit of detection at 10 to 100 pmol/hr, sc continuous administration through osmotic pumps measured up to 1 week by RIA2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179701Total clearance in Sprague-Dawley rat at 1 mg/kg, iv after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179696Testosterone-suppressive activity in Crl:CD(SD) rat assessed as number of animal with plasma testosterone level below the limit of detection at 0.01 mol/hr, sc through osmotic pumps measured after 6 days by RIA2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179690Stability of the compound in aqueous solution (JP1) assessed as residual ratio at pH 1.2 up to 2 weeks by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321526Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321536Inhibition of testosterone levels in Crl:CD(SD) rat plasma assessed as plasma testosterone level <0.04 ng/ml at 100 pmol/hr, sc administered as continuous dosing through alzet osmotic pump for 1 week by radioimmunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321542Cmax in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321530Inhibition of testosterone levels in CD(SD) rat assessed as plasma testosterone level <0.04 ng/ml at 0.003 nmol/hr, sc administered continuously for 6 days through alzet osmotic pump measured after 6 days by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179699Mean residence time in Sprague-Dawley rat at 1 mg/kg, iv after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179705Mean residence time in Sprague-Dawley rat at 1 mg/kg, sc after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321531Inhibition of testosterone levels in Crl:CD(SD) rat plasma assessed as plasma testosterone level <0.04 ng/ml at 3 pmol/hr, sc administered as continuous dosing through alzet osmotic pump for 1 week by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179698AUC (0 to 24 hrs) in Sprague-Dawley rat at 1 mg/kg, iv after 24 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321527Inhibition of testosterone levels in CD(SD) rat assessed as plasma testosterone level <0.04 ng/ml at 0.1 nmol/hr, sc administered continuously for 6 days through alzet osmotic pump measured after 6 days by radio-immunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321547Solubility of the compound in water at 20 mg/ml2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179710Toxicity in rat2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321541Total clearance in Sprague-Dawley rat plasma at 1 mg/kg, iv up to 24 hrs by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1179709Stimulation of testosterone release in Crl:CD(SD) rat assessed as testosterone AUC (0 to 4 hrs) at 0.01 to 1 nmol/kg, sc single dose2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1179691Stability of the compound in aqueous solution assessed as residual ratio at pH 3 up to 2 weeks by HPLC analysis relative to initial level2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
AID1321539AUC (0 to 24 hrs) in Sprague-Dawley rat plasma at 1 mg/kg, iv up to 24 hrs by LC/MS analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
AID1321537Inhibition of testosterone levels in Crl:CD(SD) rat plasma assessed as plasma testosterone level <0.04 ng/ml at 100 pmol/hr, sc administered as continuous dosing through alzet osmotic pump for 4 weeks by radioimmunoassay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
[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's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's13 (100.00)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: 11.74

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 Index11.74 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (15.38%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
substance p
[no description available]		2.110peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
senktide
[no description available]		2.110
leuprolide
Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		7.110oligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		3.4811monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
kisspeptin-10 protein, human
[no description available]		2.5220
kiss1 protein, human
Kisspeptins: Intercellular signaling peptides that were originally characterized by their ability to suppress NEOPLASM METASTASIS. Kisspeptins have since been found to play an important role in the neuroendocrine regulation of REPRODUCTION.		5.92122
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.1710
Cancer of Prostate
[description not available]		02.5320
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.5320
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0710