Compounds > tak-683
Page last updated: 2024-08-03 17:02:16

tak-683

Description

TAK-683: has antineoplastic activity [MeSH]

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

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
KiSS-1 receptorRattus norvegicus (Norway rat)Ki0.0001AID1179682
KiSS-1 receptorHomo sapiens (human)Ki0.0000AID1179681

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
KiSS-1 receptorRattus norvegicus (Norway rat)EC500.0013AID1179679; AID1321526
KiSS-1 receptorHomo sapiens (human)EC500.0003AID1179678; AID1321525

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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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
ISSN: 1520-4804		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

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
kisspeptin-10 protein, human
2
201420169.0high000020
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
substance p
1
peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent		2014201410.0low000010
senktide
1
2014201410.0low000010
leuprolide
1
oligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist		2014201410.0low000010
dinoprost
1
monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite		2014201410.0low100010
kiss1 protein, human
12
201220189.3high2000120
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Cancer of Prostate0
2
201420188.0high000020
Disease Models, Animal0
1
201820186.0medium000010
Prostatic Neoplasms0
2
201420188.0high000020
Sensitivity and Specificity0
1
2012201212.0medium000010

Safety/Toxicity (1)

ArticleYear
Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men.
British journal of clinical pharmacology, , Volume: 75, Issue:2		2013

Long-term Use (2)

ArticleYear
The effects of chronic subcutaneous administration of an investigational kisspeptin analog, TAK-683, on gonadotropin-releasing hormone pulse generator activity in goats.
Neuroendocrinology, , Volume: 100, Issue:2-3		2014
Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.
European journal of pharmacology, , Jul-15, Volume: 735		2014

Pharmacokinetics (2)

ArticleYear
Evaluation of pharmacokinetics/pharmacodynamics and efficacy of one-month depots of TAK-448 and TAK-683, investigational kisspeptin analogs, in male rats and an androgen-dependent prostate cancer model.
European journal of pharmacology, , Mar-05, Volume: 822		2018
Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men.
British journal of clinical pharmacology, , Volume: 75, Issue:2		2013

Dosage (2)

ArticleYear
Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.
European journal of pharmacology, , Jul-15, Volume: 735		2014
Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men.
British journal of clinical pharmacology, , Volume: 75, Issue:2		2013