Page last updated: 2024-08-07 16:22:47
Neuromedin-K receptor
A neuromedin-K receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29371]
Synonyms
NKR;
NK-3 receptor;
NK-3R;
Neurokinin B receptor;
Tachykinin receptor 3
Research
Bioassay Publications (29)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (24.14) | 18.2507 |
| 2000's | 9 (31.03) | 29.6817 |
| 2010's | 13 (44.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| substance p | Homo sapiens (human) | EC50 | 0.7930 | 1 | 1 |
| senktide | Homo sapiens (human) | EC50 | 0.0070 | 3 | 3 |
| sr 142806 | Homo sapiens (human) | Kd | 0.0129 | 7 | 7 |
| neurokinin a | Homo sapiens (human) | EC50 | 0.0530 | 1 | 1 |
| neurokinin b | Homo sapiens (human) | EC50 | 0.0060 | 1 | 1 |
| sb 223412 | Homo sapiens (human) | Kd | 0.0492 | 5 | 5 |
| eledoisin | Homo sapiens (human) | EC50 | 0.0042 | 3 | 3 |
| bufokinin | Homo sapiens (human) | EC50 | 0.0107 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| sr 142806 | Homo sapiens (human) | Ks | 0.0010 | 1 | 1 |
| sb 223412 | Homo sapiens (human) | Kb | 0.0030 | 1 | 1 |
| sb 218795 | Homo sapiens (human) | Kb | 0.0430 | 1 | 1 |
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Development of novel NK3 receptor antagonists with reduced environmental impact.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 2001
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
New quinoline NK3 receptor antagonists with CNS activity.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Discovery of novel, orally active dual NK1/NK2 antagonists.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| tachykinin receptor activity | molecular function | Combining with a tachykinin neuropeptide and transmitting the signal across the membrane by activating an associated G-protein. [GOC:ai, GOC:bf, PMID:7639617, Wikipedia:Tachykinin] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite membrane | cellular component | The portion of the plasma membrane surrounding a dendrite. [GOC:mah] |
| neuronal cell body membrane | cellular component | The plasma membrane of a neuron cell body - excludes the plasma membrane of cell projections such as axons and dendrites. [GOC:jl] |
| sperm midpiece | cellular component | The highly organized segment of the sperm flagellum which begins at the connecting piece and is characterized by the presence of 9 outer dense fibers (ODFs) that lie outside each of the 9 outer axonemal microtubule doublets and by a sheath of mitochondria that encloses the ODFs and the axoneme; the midpiece terminates about one-fourth of the way down the sperm flagellum at the annulus, which marks the beginning of the principal piece. [GOC:cjm, MP:0009831] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| sperm midpiece | cellular component | The highly organized segment of the sperm flagellum which begins at the connecting piece and is characterized by the presence of 9 outer dense fibers (ODFs) that lie outside each of the 9 outer axonemal microtubule doublets and by a sheath of mitochondria that encloses the ODFs and the axoneme; the midpiece terminates about one-fourth of the way down the sperm flagellum at the annulus, which marks the beginning of the principal piece. [GOC:cjm, MP:0009831] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| tachykinin receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by tachykinin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. Tachykinin is a short peptide with the terminal sequence (Phe-X-Gly-Leu-Met-NH2). [GOC:mah, PMID:14723970] |
| positive regulation of heart rate | biological process | Any process that activates or increases the frequency or rate of heart contraction. [GOC:dph, GOC:tb] |
| response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
| regulation of dopamine metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving dopamine. [GOC:go_curators] |
| response to cocaine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| positive regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio] |
| regulation of feeding behavior | biological process | Any process that modulates the rate, frequency or extent of the behavior associated with the intake of food. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of uterine smooth muscle contraction | biological process | Any process that increases the frequency, rate or extent of uterine smooth muscle contraction. [GOC:go_curators] |
| positive regulation of flagellated sperm motility | biological process | Any process that activates or increases the frequency, rate or extent of flagellated sperm motility. [GOC:cilia, GOC:jh2, GOC:krc, GOC:TermGenie, PMID:7513657] |