Compounds > kisspeptin-10 protein, human
Page last updated: 2024-11-13

kisspeptin-10 protein, human

Cross-References

ID SourceID
PubMed CID25240297
CHEMBL ID376756
SCHEMBL ID15930211
MeSH IDM0498593

Synonyms (28)

Synonym
chembl376756 ,
bdbm26349
(2s)-2-[(2s)-2-[(2s)-2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]butanediamido]-3-(1h-indol-3-yl)propanamido]-n-[(1s)-1-{[(1s)-1-[({[(1s)-1-{[(1s)-4-carbamimidamido-1-{[(1s)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}m
kp-10
[125i]-kp10
[125i]kp-10
gtpl1283
gtpl1281
kp10
[125i]kisspeptin-10 (human)
kisspeptin-10
human metastin 45-54
kisspeptin-10 (human)
kiss1
374675-21-5
metastin (45-54)
SCHEMBL15930211
kisspeptin 10 (human) ,
AKOS024457174
bdbm50045513
metastin (45-54) amide, human, >=95%
human kisspeptin 10f
metastin 45-54
fs1n52vs3s ,
nsc 741805
unii-fs1n52vs3s
RITKWYDZSSQNJI-INXYWQKQSA-N
EX-A5793
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
KiSS-1 receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00010.00010.00010.0001AID690938
KiSS-1 receptorRattus norvegicus (Norway rat)Ki0.00010.00010.00010.0001AID1053423; AID1179682
KiSS-1 receptorHomo sapiens (human)IC50 (µMol)1.70210.00011.55678.5100AID1053426; AID1798671; AID347797; AID570382; AID690937
KiSS-1 receptorHomo sapiens (human)Ki0.00040.00000.60023.6000AID1053424; AID1179681; AID1820167; AID277660
Neuropeptide FF receptor 1Homo sapiens (human)IC50 (µMol)0.00470.00470.20730.4100AID570383
Neuropeptide FF receptor 2Homo sapiens (human)IC50 (µMol)0.07600.07600.24300.4100AID570384
[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)0.00420.00130.00270.0042AID1179679; AID1321526
KiSS-1 receptorHomo sapiens (human)EC50 (µMol)0.00280.00000.00230.0173AID1179678; AID1321525; AID1535393; AID277661; AID347799; AID690936; AID691440
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayKiSS-1 receptorHomo sapiens (human)
neuropeptide signaling pathwayKiSS-1 receptorHomo sapiens (human)
neuropeptide signaling pathwayNeuropeptide FF receptor 1Homo sapiens (human)
biological_processNeuropeptide FF receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide FF receptor 1Homo sapiens (human)
cellular response to hormone stimulusNeuropeptide FF receptor 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide FF receptor 2Homo sapiens (human)
detection of abiotic stimulusNeuropeptide FF receptor 2Homo sapiens (human)
regulation of MAPK cascadeNeuropeptide FF receptor 2Homo sapiens (human)
cellular response to hormone stimulusNeuropeptide FF receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

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)
G protein-coupled receptor activityNeuropeptide FF receptor 1Homo sapiens (human)
protein bindingNeuropeptide FF receptor 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptide FF receptor 1Homo sapiens (human)
peptide bindingNeuropeptide FF receptor 1Homo sapiens (human)
G protein-coupled receptor activityNeuropeptide FF receptor 2Homo sapiens (human)
neuropeptide receptor activityNeuropeptide FF receptor 2Homo sapiens (human)
opioid receptor bindingNeuropeptide FF receptor 2Homo sapiens (human)
peptide bindingNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

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)
plasma membraneNeuropeptide FF receptor 1Homo sapiens (human)
ciliumNeuropeptide FF receptor 1Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 1Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 2Homo sapiens (human)
actin cytoskeletonNeuropeptide FF receptor 2Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (75)

Assay IDTitleYearJournalArticle
AID690938Binding affinity to rat KISS1R2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID691442Chemical stability of the compound after 30 mins in presence of bovine trypsin at pH 8.52012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
AID570385Selectivity index, ratio of IC50 for NPFFR1 to IC50 for GPR542011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
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
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
AID691440Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
AID1820172Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells by scintillation counting analysis2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
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
AID570384Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID570390Agonist activity at NPFFR2 expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP accumulation at up to 100 uM after 30 mins2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID347799Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
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.
AID1053416Plasma concentration in Copenhagen rat at 6 nmol/h, sc measured after 6 days by radioimmunoassay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
AID1321528Inhibition of testosterone levels in CD(SD) rat assessed as plasma testosterone level <0.04 ng/ml at 0.03 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
AID690943Metabolic stability of the compound in human serum assessed as compound residual ratio after 15 mins2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
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.
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
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
AID690937Binding affinity to human KISS1R2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID347797Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
AID690939Metabolic stability of the compound in mouse serum assessed as compound residual ratio at 0.1 mM after 1 hr2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID570386Selectivity index, ratio of IC50 for NPFFR2 to IC50 for GPR542011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID347798Ratio of IC50 of compound to IC50 of kisspeptin-10 for human GPR542008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
AID1820171Displacement of [3H]-Diprenorphine from human KOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1053426Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
AID1535394Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured immediately by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
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
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
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
AID691438Drug metabolism in mouse serum assessed as metastin(residue 46 to 54) formation within 1 min by HPLC analysis2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
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
AID691441Ratio of compound EC50 to metastin(residue 45 to 54) EC50 for human OT7T1752012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
AID1535398Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured after 60 mins by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID277660Displacement of [125]metastin from metastin receptor2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
AID570382Displacement of [125I]kisspeptin-15 from GPR542011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID690941Metabolic stability of the compound in human serum assessed as compound residual ratio after 5 mins2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID347805Stability in mouse serum within 1 hr2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
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.
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.
AID570389Agonist activity at NPFFR1 expressed in HEK293T cells co-expressing Gqi5 assessed as increase of intracellular calcium mobilization at 0.24 uM after 1 hr2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID570395Increase of GnRH release in Wistar-imamichi rat median eminence at 0.1 uM after 30 mins by double-antibody radioimmunoassay2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID1053422Metabolic stability in mouse serum assessed as compound remaining at 0.1 mM after 1 hr by HPLC analysis2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
AID1820167Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1820166Displacement of [3H]-PrRP-20 from human PrRP receptor expressed in CHO cells by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1535400Half life in Sprague-Dawley rat serum at 10 ug/ml by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID690940Drug metabolism in mouse plasma at 0.1 mM after 1 min by HPLC-ESI-MS analysis2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
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
AID690942Metabolic stability of the compound in human serum assessed as compound residual ratio after 10 mins2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID1820169Displacement of [3H]-Diprenorphine from human MOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1053423Binding affinity to rat KISS1R2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
AID570393Increase of luteinizing hormone level in Wistar-imamichi rat plasma at 0.25 nmol, administered intracerebroventricularly in preoptic area after 3 hrs measured every 6 mins by double-antibody radioimmunoassay2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID1535397Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured after 30 mins by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID691594Half life of the compound in mouse serum2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
AID1053418Suppression of testosterone in plasma of Copenhagen rat at 6 nmol/h, sc measured after 6 days by radioimmunoassay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
AID1053424Binding affinity to human KISS1R expressed in CHO cell membranes2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
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
AID691439Drug metabolism in mouse serum assessed as metastin(residue 46 to 53) formation within 1 min by HPLC analysis2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
AID1535399Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured after 120 mins by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID690936Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
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
AID691437Drug metabolism in mouse serum within 1 min by HPLC analysis2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.
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
AID1535395Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured after 5 mins by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID1820170Displacement of [3H]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID690944Half life in human serum2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
AID1535393Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID277661Activity at metastin receptor expressed in HEK293 cells by measuring calcium release2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
AID570391Agonist activity at NPFFR1 expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP accumulation at up to 100 uM after 30 mins2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID570383Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs2011ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
AID1535396Stability in Sprague-Dawley rat serum assessed as parent compound remaining at 10 ug/ml measured after 15 mins by LC-MS/MS analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
AID1820168Displacement of [125I]-43RFa from human QRFP receptor expressed in CHO cells by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1798671Receptor Binding Assay from Article 10.1021/jm800930w: \\Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase.\\2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
AID1346040Human kisspeptin receptor (Kisspeptin receptor)2001The Journal of biological chemistry, Sep-14, Volume: 276, Issue:37
The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
AID1346989Rat kisspeptin receptor (Kisspeptin receptor)2001The Journal of biological chemistry, Sep-14, Volume: 276, Issue:37
The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
AID1346040Human kisspeptin receptor (Kisspeptin receptor)2001Nature, May-31, Volume: 411, Issue:6837
Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (33.33)29.6817
2010's7 (58.33)24.3611
2020's1 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.16

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 Index12.16 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.16)

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
benzethonium chloride
benzethonium chloride : A (synthetic) quaternary ammonium salt that is benzyldimethylamine in which the nitrogen is quaternised by a 2-{2-[p-(2,4,4-trimethylpentan-2-yl)phenoxy]ethoxy}ethyl group, with chloride as the counter-ion. An antiseptic and disinfectant, it is active against a broad spectrum of bacteria, fungi, moulds and viruses.		2.0310aromatic ether;
chloride salt;
quaternary ammonium salt		antibacterial agent;
antifungal agent;
antiseptic drug;
antiviral agent;
disinfectant
enkephalin, d-penicillamine (2,5)-
Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.. DPDPE : A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond.		2.3110heterodetic cyclic peptidedelta-opioid receptor agonist
leuprolide acetate
leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0810acetate saltantineoplastic agent;
gonadotropin releasing hormone agonist
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.		2.2110oligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		2.3110morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		2.3110morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
enkephalin, ala(2)-mephe(4)-gly(5)-
[no description available]		2.3110peptide
phenylalanyl-leucyl-phenylalanyl-glutaminyl-prolyl-glutaminyl-arginyl-phenylalaninamide
[no description available]		2.3110
nociceptin
[no description available]		2.3110organic molecular entity;
polypeptide		human metabolite;
rat metabolite
tak-683
TAK-683: has antineoplastic activity		2.5220
RF9
[no description available]		2.5320dipeptidekisspeptin receptor agonist;
neuropeptide FF receptor agonist;
neuropeptide FF receptor antagonist
ConditionIndicatedRelationship StrengthStudiesTrials
Metastase
[description not available]		02.4120
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.4120
Allodynia
[description not available]		02.3110
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