Page last updated: 2024-08-07 16:10:13
Substance-K receptor
A substance-K receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P21452]
Synonyms
SKR;
NK-2 receptor;
NK-2R;
Neurokinin A receptor;
Tachykinin receptor 2
Research
Bioassay Publications (34)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (20.59) | 18.2507 |
| 2000's | 19 (55.88) | 29.6817 |
| 2010's | 8 (23.53) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (65)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| sr 142806 | Homo sapiens (human) | Log Ki | 0.0370 | 1 | 1 |
| neurokinin a | Homo sapiens (human) | KD/Ki | 0.0063 | 15 | 15 |
| men 11558 | Homo sapiens (human) | KD/Ki | 0.4927 | 23 | 23 |
| men 11420 | Homo sapiens (human) | KD/Ki | 0.4623 | 23 | 23 |
The design and synthesis of novel NK1/NK2 dual antagonists.Bioorganic & medicinal chemistry letters, , Oct-16, Volume: 10, Issue:20, 2000
L-tryptophan urea amides as NK1/NK2 dual antagonists.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
L-tryptophan urea amides as NK1/NK2 dual antagonists.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.Journal of medicinal chemistry, , Apr-29, Volume: 37, Issue:9, 1994
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
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
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
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
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
Toward fluorescent probes for G-protein-coupled receptors (GPCRs).Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
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
Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
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
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
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
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
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. 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
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
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
Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionBioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
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 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| substance K receptor activity | molecular function | Combining with substance K, the peptide His-Lys-Thr-Asp-Ser-Phe-Val-Gly-Leu-Met, to initiate a change in cell activity. [GOC:mah, ISBN:0198506732] |
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] |
| sperm flagellum | cellular component | A microtubule-based flagellum (or cilium) that is part of a sperm, a mature male germ cell that develops from a spermatid. [GOC:cilia, GOC:sart, PMID:8441407] |
| sperm head | cellular component | The part of the late spermatid or spermatozoon that contains the nucleus and acrosome. [PMID:22797892, PMID:24665388] |
| 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 |
|---|
| 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] |
| 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] |
Involved In
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|
| muscle contraction | biological process | A process in which force is generated within muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. [GOC:ef, GOC:mtg_muscle, ISBN:0198506732] |
| 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 acetylcholine secretion, neurotransmission | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of acetylcholine. [GOC:ef] |
| intestine smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. This process occurs in the intestine. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. The intestine is the section of the alimentary canal from the stomach to the anal canal. It includes the large intestine and small intestine. [GOC:mtg_muscle, MA:0001539, MSH:D007422] |
| negative regulation of luteinizing hormone secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of luteinizing hormone. [GOC:mah] |
| operant conditioning | biological process | Learning to anticipate future events on the basis of past experience with the consequences of one's own behavior. [PMID:14662373] |
| positive regulation of vascular permeability | biological process | Any process that increases the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
| positive regulation of monoatomic ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of charged atoms or small charged molecules into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
| positive regulation of smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| response to electrical stimulus | 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 an electrical stimulus. [GOC:ai] |
| prolactin secretion | biological process | The regulated release of prolactin, a peptide hormone that stimulates lactation, from secretory granules in the anterior pituitary. [GOC:mah, ISBN:0198506732] |
| 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] |