Page last updated: 2024-12-05

azetidyl-2-carboxylic acid

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

Description

Azetidyl-2-carboxylic acid, also known as azetidine-2-carboxylic acid, is a non-proteinogenic amino acid. It is a cyclic beta-amino acid with a four-membered ring structure. It is synthesized by a variety of methods, including the ring-closing metathesis of an N-protected allylglycine derivative. Azetidyl-2-carboxylic acid has been studied for its potential biological activity, and has been shown to be a potent inhibitor of certain enzymes. It has also been explored as a building block for the synthesis of novel peptides and pharmaceuticals.'

azetidyl-2-carboxylic acid: a proline analog (with 4-membered ring in place of 5); a toxic non-protein amino acid that is misincorporated into protein in place of proline; induces nonfunctional heat-shock proteins; inhibits acquired thermotolerance; RN given refers to (L)-isomer; found in beets and Liliaceae [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(S)-azetidine-2-carboxylic acid : The (S)-enantiomer of azetidine-2-carboxylic acid. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

azetidinecarboxylic acid : A member of the class of azetidines that is azetidine substituted by at least one carboxy group at unspecified position. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
LiliaceaefamilyA monocot family within the order Liliales.[MeSH]LiliaceaeA monocot family within the order Liliales.[MeSH]

Cross-References

ID SourceID
PubMed CID16486
CHEMBL ID1165239
CHEBI ID6198
SCHEMBL ID20296
MeSH IDM0236326

Synonyms (84)

Synonym
AC-5699
LOPAC0_000023
l-azetidine-2-carboxylic acid
EU-0100023
l-azetidine-2-carboxylic acid, >=99%
(2s)-azetidine-2-carboxylic acid
CHEBI:6198 ,
(s)-2-azetidinecarboxylic acid
(s)-azetidine-2-carboxylic acid
azetidinecarboxylic acid
2-azetidinecarboxylic acid, l-
einecs 218-362-5
acide l-azetidine-2-carboxylic [french]
azetidine-2-carboxylic acid, l-
2-azetidinecarboxylic acid, (s)-
hsdb 3465
(l)-azetidine-2-carboxylic acid
l-azetidine 2-carboxylic acid
azetidyl-2-carboxylic acid
C08267
(s)-(-)-azetidine-2-carboxylic acid
2133-34-8
NCGC00093546-01
NCGC00093546-02
A 0760
A1043
l-trimethyleneimine-2-carboxylic acid
NCGC00093546-03
(s)-(-)-2-azetidinecarboxylic acid
CHEMBL1165239 ,
A4601
azetidine-2-carboxylic acid;(s)-azetidine-2-carboxylic acid
AKOS005254687
HMS3260E07
(2s)azetidine-2-carboxylic acid
ST059592
acide l-azetidine-2-carboxylic
unii-5gz3e0l9zu
5gz3e0l9zu ,
AKOS006239010
CCG-204119
bdbm50357225
AM20090185
LP00023
2-azetidinecarboxylic acid, (2s)-
l-2-azetidinecarboxylic acid
azetidyl-2-carboxylic acid [hsdb]
(s)-(-)-2-azetidine carboxylic acid
(-)-azetidinecarboxylic acid
gtpl4686
(s)-(-) azetidine-2-carboxylic acid
SCHEMBL20296
tox21_500023
NCGC00260708-01
(s)-2-azetidinecarboxyic acid
(s)-(-)-2-azetidine-carboxylic acid
azetidine-2-(s)-carboxylic acid
azeoh
l-azetidine-2carboxylic acid
l--azetidine-2-carboxylic acid
l-azeoh
2-(s)-azetidinecarboxylic acid
azetidine-2(s)-carboxylic acid
(s)-2-azetidine carboxylic acid
l-azetidine-2caboxylic acid
DTXSID0044020
W-107562
mfcd00005166
SR-01000075656-1
sr-01000075656
(s)-azetidin-2-carbonsaure
(s)-2-azetidinecarboxylic acid;h-aze-oh
02a ,
CS-0031389
DS-16309
(s)-l-azetidine-2-carboxylic acid
Q793715
h-aze(2)-oh
SDCCGSBI-0050012.P002
NCGC00093546-04
HY-W050044
l-azetidine-2-carboxylic acid is known as a proline analog.
EN300-85821
(s)-azetidine-2-carboxylicacid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"In the retina, the activation of metabotropic glutamate receptors (mGluRs) reduces the toxic effect of N-methyl-D-aspartate (NMDA)."( A derivative of a rigid glutamate analog protects the retina from excitotoxicity.
Arban, R; Fadda, E; Kozikowski, AP; Lipartiti, M; Manev, H; Siliprandi, R, 1994
)
0.29
" The incidence of adverse events was similar in the O/A combination groups and the monotherapy groups."( A randomized, double-blind, four-arm parallel-group study of the efficacy and safety of azelnidipine and olmesartan medoxomil combination therapy compared with each monotherapy in Japanese patients with essential hypertension: the REZALT study.
Kuramoto, K; Ogihara, T; Saruta, T; Shimada, K, 2009
)
0.35
"Hsp104 is an AAA+ protein disaggregase, which can be potentiated via diverse mutations in its autoregulatory middle domain (MD) to mitigate toxic misfolding of TDP-43, FUS, and α-synuclein implicated in fatal neurodegenerative disorders."( Mining Disaggregase Sequence Space to Safely Counter TDP-43, FUS, and α-Synuclein Proteotoxicity.
Carman, PJ; Gambogi, C; Gates, SN; Gurpinar, E; Hernandez Murillo, OA; Hesketh, CD; Jackrel, ME; Lin, J; Mack, KL; Rizo, AN; Shorter, J; Southworth, DR; Stillman, J; Sudesh, S; Sweeny, EA; Tariq, A; Weitzman, R; Yee, K; Yokom, AL, 2019
)
0.51

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic results indicated that the plasma half-life (t1/2) of amlodipine was 38."( Azelnidipine and amlodipine: a comparison of their pharmacokinetics and effects on ambulatory blood pressure.
Hirai, A; Ichikawa, S; Kanada, S; Kuramoto, K; Nakachi, T; Ogihara, T, 2003
)
0.32
"23) L/h, respectively; peak plasma concentration Cmax were (8."( Determination of azelnidipine by LC-ESI-MS and its application to a pharmacokinetic study in healthy Chinese volunteers.
Fan, HW; Hu, Q; Ji, HJ; Xiao, DW; Zhou, XH; Zhu, YB; Zou, JJ, 2008
)
0.35
" In conclusion, the effects of olmesartan medoxomil and azelnidipine were modestly correlated with pharmacokinetic profiles, and the pre-treatment PRA level could be a useful determinant of responsiveness in selecting olmesartan medoxomil and azelnidipine."( Comparative pharmacodynamics of olmesartan and azelnidipine in patients with hypertension: a population pharmacokinetic/pharmacodynamic analysis.
Arakawa, K; Kuramoto, K; Tanigawara, Y; Yoshihara, K, 2009
)
0.35
" Finally, the method was successfully applied to a clinical pharmacokinetic study in human after a single oral administration of azelnidipine 8 mg."( A liquid chromatography-tandem mass spectrometric assay for the antihypertensive agent azelnidipine in human plasma with application to clinical pharmacokinetics studies.
Fang, Z; Gao, Y; Li, B; Liu, D; Lou, H; Wang, H; Zhao, H; Zhu, B, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
"The aim of this study was to compare the effects between calcium channel blockers and diuretics when used in combination with angiotensin II receptor blocker on aortic systolic blood pressure (BP) and brachial ambulatory systolic BP."( Differential effects between a calcium channel blocker and a diuretic when used in combination with angiotensin II receptor blocker on central aortic pressure in hypertensive patients.
Eguchi, K; Ishikawa, J; Kario, K; Matsui, Y; Miyashita, H; O'Rourke, MF; Shimada, K, 2009
)
0.35
" In this study, the efficacy of treatment using an angiotensin II receptor antagonist (ARB) combined with a calcium channel blocker (CCB) or a diuretic was compared from multiple perspectives in patients with hypertension."( Angiotensin-II receptor antagonist combined with calcium channel blocker or diuretic for essential hypertension.
Akabane, T; Ishimitsu, T; Masuda, T; Matsuoka, H; Minami, J; Numabe, A; Okamura, A, 2009
)
0.35
"A thiazide diuretic used in combination with benazepril is superior to amlodipine plus benazepril in reducing albuminuria in hypertensive patients with diabetes."( Kidney-protective effects of azelnidipine versus a diuretic in combination with olmesartan in hypertensive patients with diabetes and albuminuria: a randomized study.
Dohi, Y; Hirota, H; Isaka, N; Ito, M; Kato, T; Kimura, G; Kojima, M; Machida, H; Makino, K; Miyagawa, K; Mizubayashi, R; Mizuno, O; Nakatani, K; Okamoto, S; Okubo, S; Okura, T; Takeuchi, M, 2013
)
0.39
"Azelnidipine is equally effective as a thiazide diuretic in reducing urinary albumin when used in combination with olmesartan."( Kidney-protective effects of azelnidipine versus a diuretic in combination with olmesartan in hypertensive patients with diabetes and albuminuria: a randomized study.
Dohi, Y; Hirota, H; Isaka, N; Ito, M; Kato, T; Kimura, G; Kojima, M; Machida, H; Makino, K; Miyagawa, K; Mizubayashi, R; Mizuno, O; Nakatani, K; Okamoto, S; Okubo, S; Okura, T; Takeuchi, M, 2013
)
0.39

Bioavailability

ExcerptReferenceRelevance
" As these phytosiderophores have the ability to form thermodynamically stable complexes with other metal cations present in the growing medium, they have also been implicated in the transport and bioavailability of these metals in the environment."( Anion exchange liquid chromatography--inductively coupled plasma-mass spectrometry detection of the Co2+, Cu2+, Fe3+ and Ni2+ complexes of mugineic and deoxymugineic acid.
Bakkaus, E; Collins, RN; Gouget, B; Morel, JL, 2006
)
0.33
" Bioavailability of Fe from the high NA grain, as measured by ferritin synthesis in an in vitro Caco-2 cell model that simulates the human digestive system, was twice as much as that of the control line."( Nicotianamine, a novel enhancer of rice iron bioavailability to humans.
Ai, C; Bei, X; Cheng, Z; Glahn, RP; Jiang, X; Lei, XG; Miller, DD; Shou, H; Welch, RM; Zheng, L; Zheng, Y, 2010
)
0.36
"Impaired wound healing in diabetes is associated with decreased nitric oxide (NO) bioavailability in wound tissue."( Azelnidipine, a new calcium channel blocker, promotes skin wound healing in diabetic rats.
Amirghofran, Z; Bagheri, M; Jahromi, BM; Mirkhani, H; Noorafshan, A; Solhjou, Z; Zamani, A, 2011
)
0.37
"The metal chelator nicotianamine promotes the bioavailability of Fe and reduces cellular Fe toxicity."( Nicotianamine functions in the Phloem-based transport of iron to sink organs, in pollen development and pollen tube growth in Arabidopsis.
Abadía, J; Bauer, P; Fink-Straube, C; Rellán-Álvarez, R; Schuler, M, 2012
)
0.38
" However, phytate is only part of the answer to the multifaceted bioavailability question, albeit an important one."( Zn and Fe biofortification: the right chemical environment for human bioavailability.
Clemens, S, 2014
)
0.4
"Iron bioavailability in unleavened white and wholegrain bread made from two commercial wheat varieties was assessed by measuring ferritin production in Caco-2 cells."( Iron bioavailability in two commercial cultivars of wheat: comparison between wholegrain and white flour and the effects of nicotianamine and 2'-deoxymugineic acid on iron uptake into Caco-2 cells.
Eagling, T; Fairweather-Tait, SJ; Shewry, PR; Wawer, AA; Zhao, FJ, 2014
)
0.4
" Biofortification is a micronutrient intervention aimed at increasing the density and bioavailability of essential vitamins and minerals in staple crops; Fe biofortification of wheat has proved challenging."( Metabolic engineering of bread wheat improves grain iron concentration and bioavailability.
Beasley, JT; Bonneau, JP; Callahan, DL; Glahn, RP; Johnson, AAT; Lombi, E; Moreno-Moyano, LT; Sánchez-Palacios, JT; Tako, E, 2019
)
0.51
"Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy."( Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength.
Abd El Rehim, RT; El-Gazayerly, ON; El-Helaly, SN; Rashad, AA, 2019
)
0.51
"Azelnidipine, dihydropyridine based calcium channel blocker has been used for treating ischemic heart disease and cardiac remodeling after myocardial infarction but it is having a low bioavailability due to its poor solubility."( Improved bioavailability of Azelnidipine gastro retentive tablets-optimization and in-vivo assessment.
Avari, JG; Gaikwad, SS, 2019
)
0.51
" The main challenge was the poor bioavailability of azelnidipine due to its poor aqueous solubility and first-pass effect."( Chronological Delivery of Antihypertensive Drugs in Bilayered Core-in-Cup Buccoadhesive Tablets: In Vitro and In Vivo Evaluation.
Abd El Rehim, RT; El-Gazayerly, ON; Nageeb El-Helaly, S; Rashad, AA, 2019
)
0.51
" Nicotianamine (NA) is a natural chelator of Fe, zinc (Zn) and other metals in higher plants and NA-chelated Fe is highly bioavailable in vitro."( Nicotianamine-chelated iron positively affects iron status, intestinal morphology and microbial populations in vivo (Gallus gallus).
Beasley, JT; Bonneau, JP; Glahn, RP; Johnson, AAT; Kolba, N; Koren, O; Ozeri, L; Tako, E, 2020
)
0.56
" It is unclear how important plant-derived chelators, such as nicotianamine (NA), an organic small molecule that is ubiquitous in crops, vegetables, and various other foods, contribute to iron bioavailability in mammals."( Iron uptake mediated by the plant-derived chelator nicotianamine in the small intestine.
Morimoto, S; Murata, Y; Namba, K; Sakamoto, N; Watanabe, T; Yoshida, M,
)
0.13
"Iron (Fe) is an essential nutrient, but is poorly bioavailable because of its low solubility in alkaline soils; this leads to reduced agricultural productivity."( Development of a mugineic acid family phytosiderophore analog as an iron fertilizer.
Aung, MS; Chiba, Y; Fujino, H; Fukushima, K; Kanaki, M; Kobayashi, K; Kobayashi, T; Masuda, H; Mera, A; Mukaiyama, H; Murata, Y; Nakanishi, H; Nakayama, A; Namba, K; Nishio, S; Nishizawa, NK; Sasaki, S; Shrestha, BB; Suzuki, M; Takeuchi, M; Tanino, K; Tsugawa, R; Urabe, A; Watanabe, T, 2021
)
0.62
" Here we describe multi-location confined field trial (CFT) evaluation of a low-copy transgenic CE-OsNAS2 wheat event (CE-1) over 3 years and demonstrate higher concentrations of NA, DMA, Fe, and Zn in CE-1 wholemeal flour, white flour, and white bread and higher Fe bioavailability in CE-1 white flour relative to a null segregant (NS) control."( Multi-year field evaluation of nicotianamine biofortified bread wheat.
Appels, R; Beasley, JT; Bonneau, JP; Callahan, DL; Glahn, RP; Howell, KS; Johnson, AAT; Moreno-Moyano, LT; Tako, E; Taylor, J, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" At the end of the dosing period, hemodynamic changes were examined using the radioactive microsphere technique."( Hemodynamic changes following long-term administration of CS-905, a novel dihydropyridine calcium blocker, in conscious SHR.
Koike, H; Miyake, S; Miyamoto, M; Nishino, H; Oizumi, K; Sada, T; Shiga, H, 1990
)
0.28
" The analysis of dose-response and time-course Ni treatments have revealed that the exposure to Ni triggers the accumulation of NA in the roots."( Root-to-shoot long-distance circulation of nicotianamine and nicotianamine-nickel chelates in the metal hyperaccumulator Thlaspi caerulescens.
Briat, JF; Czernic, P; Gendre, D; Lebrun, M; Lobinski, R; Mari, S; Ouerdane, L; Pianelli, K, 2006
)
0.33
" The grass Deschampsia cespitosa was dosed with either Ni or Cd or pulsed with exogenous ABA."( Chelator profiling in Deschampsia cespitosa (L.) Beauv. Reveals a Ni reaction, which is distinct from the ABA and cytokinin associated response to Cd.
Coates, KE; Emery, RJ; Galer, AL; Hayward, AR; Hutchinson, TC, 2013
)
0.39
"We analyzed the self-measured home BP data (measured in the morning and at bedtime) from this 16-week prospective observational study to clarify the effect of morning dosing of azelnidipine (mean [± standard deviation] maximum dose 14."( Study of sustained blood pressure-lowering effect of azelnidipine guided by self-measured morning and evening home blood pressure: subgroup analysis of the At-HOME study.
Hiramatsu, K; Kario, K; Komiya, M; Shimada, K; Shiosakai, K; Shirayama, M; Takahashi, M; Uehara, Y, 2013
)
0.39
" Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclinical species."( Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abibi, A; Aguirre, AL; Bousquet, P; Gintant, G; Harris, CM; Hobson, AD; Kebede, T; Kim, Y; Konopacki, DB; Larson, K; Maull, JW; Moore, NS; Sarris, KK; Shi, D; Shrestha, A; Tang, X; Turner, SC; van der Kam, EL; Zhang, P, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
azetidine-2-carboxylic acidAn azetidinecarboxylic acid that is azetidine substituted by a carboxy group at position 2. It is a plant non-protein amino acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bloom syndrome protein isoform 1Homo sapiens (human)Potency1.00000.540617.639296.1227AID2364; AID2528
lamin isoform A-delta10Homo sapiens (human)Potency5.62340.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
monoatomic ion transportProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid transportProton-coupled amino acid transporter 1Homo sapiens (human)
taurine transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
proline transportProton-coupled amino acid transporter 1Homo sapiens (human)
alanine transportProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid import across plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
glycine transportProton-coupled amino acid transporter 1Homo sapiens (human)
proline transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
proton transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
L-alanine transportProton-coupled amino acid transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
amino acid:proton symporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
proline:proton symporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
taurine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
protein bindingProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
alanine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
L-alanine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
L-proline transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
glycine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
lysosomal membraneProton-coupled amino acid transporter 1Homo sapiens (human)
endoplasmic reticulumProton-coupled amino acid transporter 1Homo sapiens (human)
plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
apical plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
vacuolar membraneProton-coupled amino acid transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID52231Influx of calcium in Cerebellar Granule Cells of rat after 10 min of incubation with compound1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
AID487208Inhibition of GAT3-mediated [3H]GABA uptake in bovine brain stem2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
AID52242Stimulation caused by aspartate in Cerebellar Granule Cells over basal stimulation1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
AID487206Inhibition of GAT1-mediated [3H]GABA uptake in bovine frontal cortex2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
AID52232Influx of calcium in Cerebellar Granule Cells of rat after 10 min of incubation with compound and 10 uM aspartate1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
AID630741Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Three-dimensional quantitative structure-activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1).
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (588)

TimeframeStudies, This Drug (%)All Drugs %
pre-199079 (13.44)18.7374
1990's71 (12.07)18.2507
2000's186 (31.63)29.6817
2010's222 (37.76)24.3611
2020's30 (5.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.30

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 Index8.30 (24.57)
Research Supply Index6.48 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials49 (8.17%)5.53%
Reviews29 (4.83%)6.00%
Case Studies3 (0.50%)4.05%
Observational2 (0.33%)0.25%
Other517 (86.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]