Page last updated: 2024-11-11

zd 6021

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

Description

ZD 6021: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9852253
CHEMBL ID129683
SCHEMBL ID7673763
MeSH IDM0393587

Synonyms (15)

Synonym
zd 6021
3-cyano-n-[(2s)-2-(3,4-dichlorophenyl)-4-[4-[2-[(s)-methylsulfinyl]phenyl]piperidin-1-yl]butyl]-n-methylnaphthalene-1-carboxamide
gtpl2109
CHEMBL129683 ,
zd-6021
zd6021
bdbm50279775
(s)-3-cyano-naphthalene-1-carboxylic acid {2-(3,4-dichloro-phenyl)-4-[4-(2-methanesulfinyl-phenyl)-piperidin-1-yl]-butyl}-methyl-amide
3-cyano-naphthalene-1-carboxylic acid ((s)-2-(3,4-dichloro-phenyl)-4-{4-[2-((s)-methanesulfinyl)-phenyl]-piperidin-1-yl}-butyl)-methyl-amide
SCHEMBL7673763
n-[(s)-2-(3,4-dichlorophenyl)-4-[4-[(s)-2-methylsulfinylphenyl]-1-piperidinyl]butyl]-n-methyl-3-cyano-1-naphthamide
SJHZTGDJTIZMSK-KPRDSAADSA-N
255049-08-2
Q27089285
cid 9852253
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-K receptorHomo sapiens (human)Ki0.00060.00011.92429.7930AID211719; AID211874
Substance-P receptorHomo sapiens (human)Ki0.00010.00000.79368.7470AID208570; AID208581
Neuromedin-K receptorHomo sapiens (human)Ki0.07400.00020.05430.9250AID212245; AID212251
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

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)
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwayNeuromedin-K receptorHomo sapiens (human)
positive regulation of heart rateNeuromedin-K receptorHomo sapiens (human)
response to estradiolNeuromedin-K receptorHomo sapiens (human)
regulation of dopamine metabolic processNeuromedin-K receptorHomo sapiens (human)
response to cocaineNeuromedin-K receptorHomo sapiens (human)
positive regulation of blood pressureNeuromedin-K receptorHomo sapiens (human)
regulation of feeding behaviorNeuromedin-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionNeuromedin-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilityNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

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)
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingNeuromedin-K receptorHomo sapiens (human)
tachykinin receptor activityNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

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)
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
dendrite membraneNeuromedin-K receptorHomo sapiens (human)
neuronal cell body membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
AID208101Effective dose concentration required for In vivo binding affinity towards Tachykinin receptor 1 after oral administration in presence of agonist ASMSP in guinea pig pulmonary tissue in lung plasma extravation assay2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID13141Bioavailability by oral administration at a dose of 100 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID208570Binding affinity against human cloned Tachykinin receptor 1 expressed in MEL cells2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID11626Maximum concentration by oral administration at a dose of 100 umol/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID212245Binding affinity against human cloned Tachykinin receptor 3 expressed in MEL cells2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID145489In vivo efficacy expressed as dose ratio for bronchoconstriction induced by ASMSP as agonist for NK1 receptor in anesthetized guinea pig2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID26480Bioavailability in rat (dose 1-10 uM/kg i.v.)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID9910Volume distribution at a dose of 1 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID208103Effective dose of concentration required for In vivo potency (ED50 ratio for Tachykinin receptor 1 in presence and absence of antagonist) in guinea pig PMM after intravenous administration at a dose 10 uM/Kg2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID10888Tmax by oral administration at a dose of 100 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211330Binding constant towards tachykinin receptor 1 using ASMSP as agonist on rabbit pulmonary artery tissues.2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211885Binding constant towards Tachykinin receptor 2 using NKA as agonist on human bronchus2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211905Tested for the binding affinity towards tachykinin receptor 2 (NK2) in rabbit pulmonary artery tissue2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID12148Area under curve by intravenous administration at a dose of 10 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID26479Bioavailability in dog (dose 1-10 uM/kg i.v.)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID8921Maximum concentration by oral administration at a dose of 10 umol/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211512Effective dose of concentration required for In vivo potency (ED50 ratio for Tachykinin receptor 2 in presence and absence of antagonist) in guinea pig PMM after intravenous administration at a dose 10 uM/Kg2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID212251Inhibition of binding of [125I]MPNI to human Tachykinin receptor 3 (NK3) expressed in mouse erythroleukemia cells2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID8138Area under curve by oral administration at a dose of 10 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211719Binding affinity against human cloned Tachykinin receptor 2 expressed in MEL cells2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID208581Inhibition of binding of [3H]SP to Tachykinin receptor 1 of human tachykinin receptor expressed in mouse erythroleukemia cells2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID10275Half life period at a dose of 1 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211874Inhibition of binding of [3H]NKA to human Tachykinin receptor 2 (NK2) expressed in mouse erythroleukemia cells2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID9743Tmax by oral administration at a dose of 10 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID208595Binding constant towards Tachykinin receptor 1 using ASMSP as agonist on human pulmonary artery tissues2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211511Effective dose of concentration required for In vivo potency (ED50 ratio for Tachykinin receptor 2 (NK2) in presence and absence of antagonist) in guinea pig PMM after oral administration at a dose 30 uM/Kg2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID211901Binding constant towards Tachykinin receptor 2 using BANK as agonist on rabbit pulmonary artery tissues.2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID10797Plasma clearance in rat at a dose of 10 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID10796Plasma clearance in dog at a dose of 1 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211332In vitro binding affinity towards Tachykinin receptor 1 was determined using rabbit pulmonary artery tissues2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
AID208102Effective dose of concentration required for In vivo potency (ED50 ratio for NK1 in presence and absence of antagonist) in guinea pig PMM after oral administration at a dose 30 uM/Kg2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID10285Half-life period by oral administration at a dose of 10 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID12484Half life period at a dose of 10 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID145618In vivo efficacy expressed as dose ratio for bronchoconstriction induced by BANK as agonist for NK2 receptor in anesthetized guinea pig at 30 uM/kg dose by oral administration2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211903In vitro binding affinity towards Tachykinin receptor 2 using rabbit pulmonary artery tissues2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
AID8357Bioavailability by oral administration at a dose of 10 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID11124Volume distribution at a dose of 10 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID12149Area under curve by oral administration at a dose of 100 uM/kg in rat was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID12485Half life period by oral administration at a dose of 100 uM/kg in rat was determined; ND is not determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID8137Area under curve by intravenous administration at a dose of 1 uM/kg in dog was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Discovery of novel, orally active dual NK1/NK2 antagonists.
AID211509Effective dose concentration required for In vivo binding affinity towards Tachykinin receptor 2 (NK2) receptor after oral administration in presence of agonist ASMSP in guinea pig pulmonary tissue in lung plasma extravation assay2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID211334Tested for the binding affinity towards tachykinin receptor 1 (NK1) in rabbit pulmonary artery tissue2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
AID1346346Human NK1 receptor (Tachykinin receptors)2001The Journal of pharmacology and experimental therapeutics, Jul, Volume: 298, Issue:1
Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors.
[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's5 (100.00)29.6817
2010's0 (0.00)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: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

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]