Page last updated: 2024-12-04

3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid

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Description

3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid: structure given in first source; NMDA receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1228
CHEMBL ID22304
SCHEMBL ID167788
MeSH IDM0144363

Synonyms (62)

Synonym
EU-0100322
(+/-)-cpp, solid
LOPAC0_000322
c8h17n2o5p
dl-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid
2-piperazinecarboxylic acid, 4-(3-phosphonopropyl)-, (+-)-
3-2-cpp
4-(3-phosphonopropyl)-2-piperazinecarboxylic acid
3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid
2-piperazinecarboxylic acid, 4-(3-phosphonopropyl)-
NCGC00024482-02
(?)-cpp
NCGC00024482-03
100828-16-8
NCGC00015179-03
( inverted question mark)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid
( inverted question mark)-cpp
C-104
NCGC00015179-05
CHEMBL22304 ,
(+/-)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid
4-(3-phosphonopropyl)piperazine-2-carboxylic acid
4-(3-phosphono-propyl)-piperazine-2-carboxylic acid (cpp)
(cpp)4-(3-phosphono-propyl)-piperazine-2-carboxylic acid
3-phosphono-1-propyl-piperazine-2-carboxylic acid(dl-cpp)
4-(3-phosphono-propyl)-piperazine-2-carboxylic acid
bdbm50002360
HMS3261A05
CCG-204417
NCGC00015179-04
98y1i8zd4m ,
unii-98y1i8zd4m
(rs)-cpp
(+/-)-cpp
LP00322
(+)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphoric acid
gtpl4082
[3h]cpp
SCHEMBL167788
(y)-cpp
tox21_500322
NCGC00261007-01
carboxypeptidase p
9075-64-3
(rs)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid
AKOS024456756
3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate
cpp, (+/-)-
J-510489
SR-01000075428-3
SR-01000075428-1
sr-01000075428
CUVGUPIVTLGRGI-UHFFFAOYSA-N
HB0036
(+/-)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonicacid
SDCCGSBI-0050310.P002
4-(3-phosphonopropyl)piperazine-2-carboxylic acid.
C-175
Q27272147
DTXSID10905774
CS-0020444
HY-100797

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The half-life of [3H]CPP varied little (mean range 94-191 min) irrespective of the route of administration or the level of sampling."( CSF and plasma pharmacokinetics of the NMDA receptor antagonist CPP after intrathecal, extradural and i.v. administration in anaesthetized pigs.
Gordh, T; Halldin, M; Hartvig, P; Karlsten, R; Kristensen, JD, 1995
)
0.29

Dosage Studied

ExcerptRelevanceReference
"03-3 mg/kg did not produce changes in the midazolam dose-response curve for either unpunished or punished responding."( NMDA antagonists: lack of antipunishment effect in squirrel monkeys.
Balster, RL; Jortani, SA; Mansbach, RS; Willetts, J, 1991
)
0.28
" Addition of GTP resulted in a rightward shift in the glutamate dose-response curve and a decrease in the maximum level of stimulation."( Guanine nucleotide modulation of [3H]TCP binding to the NMDA receptor complex.
Compton, RP; Hood, WF; Monahan, JB; Thomas, JW, 1990
)
0.28
" Two potent, selective and competitive NMDA antagonists, cis-4-(phosphonomethyl)-2-piperidine-carboxylic acid (CGS 19755) and 4-(3-phosphonopropyl)-2-piperazine-carboxylic acid (CPP), were characterized in the gerbil ischemia model with respect to dose-response and time course effects."( The N-methyl-D-aspartate antagonists CGS 19755 and CPP reduce ischemic brain damage in gerbils.
Boast, CA; Etienne, PE; Gerhardt, SC; Lehmann, J; Liebman, JM; Pastor, G, 1988
)
0.27
") caused vacuolation in cortical pyramidal neurons in the posterior cingulate cortex four hours after dosing and this dose of CGP 37849 caused a pattern of limbic glucose metabolism activation similar to that seen after dizocilpine."( Competitive as well as uncompetitive N-methyl-D-aspartate receptor antagonists affect cortical neuronal morphology and cerebral glucose metabolism.
Hargreaves, RJ; Hill, RG; Iversen, LL; Rigby, M; Smith, D, 1993
)
0.29
" In the tail-flick test, the antinociceptive effect was attenuated at higher doses, resulting in a bell-shaped dose-response relationship."( The NMDA antagonist 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) has antinociceptive effect after intrathecal injection in the rat.
Berge, OG; Gordh, T; Karlsten, R; Kristensen, JD, 1994
)
0.61
" The objective of this study was to conduct a dose-response analysis of the effects of (+)MK-801 on stereotyped behavior, ataxia, locomotor activity, and righting reflex latency in guinea pig."( A dose-response analysis of the behavioral effects of (+)MK-801 in guinea pig: comparison with CPP.
Darlington, CL; Jerram, AH; Smith, PF, 1996
)
0.29
" Our results support the hypothesis that SS and LS mice differ in initial sensitivity to NMDAR antagonists and suggest that the line differences in the dose-response relationships for MK-801- and CPP-induced locomotor activity are qualitatively similar to those reported for ethanol."( Differences in NMDA receptor antagonist-induced locomotor activity and [3H]MK-801 binding sites in short-sleep and long-sleep mice.
Simpson, VJ; Velardo, MJ; Zahniser, NR, 1998
)
0.3
" The noncompetitive antagonist MK-801 and a glycine-site blocker were equally neuroprotective in both normal and reduced conditions, but there was a significant rightward shift in the dose-response curves of the competitive antagonists APV and CPP and the uncompetitive antagonist memantine."( Reducing conditions significantly attenuate the neuroprotective efficacy of competitive, but not other NMDA receptor antagonists in vitro.
Eshak, M; Iannotti, F; Pringle, AK; Self, J, 2000
)
0.31
" Estrogen treatment shifted the dose-response curve to CPP in both experiments."( Estrogen treatment alleviates NMDA-antagonist induced hippocampal LTP blockade and cognitive deficits in ovariectomized mice.
Gureviciene, I; Puoliväli, J; Pussinen, R; Tanila, H; Wang, J; Ylinen, A, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.66840.003245.467312,589.2998AID2517
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency2.83710.125919.1169125.8920AID2353; AID2549
regulator of G-protein signaling 4Homo sapiens (human)Potency0.59670.531815.435837.6858AID504845
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency0.22390.28189.721235.4813AID2326
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency5.98900.035520.977089.1251AID504332
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.35480.010039.53711,122.0200AID1479
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency0.84920.425612.059128.1838AID504536
M-phase phosphoprotein 8Homo sapiens (human)Potency89.12510.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency0.00500.891312.067628.1838AID1487
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.07570.060110.745337.9330AID485368
[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)
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki100.00000.00000.41052.7800AID92947
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.600310.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki100.00000.00380.79754.1000AID91469
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.630610.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)29.06830.00061.525710.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.747210.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.741110.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.741110.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)29.06830.00071.741110.0000AID143072; AID144462; AID144605; AID144621; AID144892; AID144907; AID144911; AID144970; AID145097; AID145098
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID144462Displacement of [3H]CPP from rat synaptic membrane glutamate NMDA receptor2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID229464Equipotent molar ratio relative to D-AP5 (1.0) on neonatal rat motoneurones.1994Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
Synthesis, NMDA receptor antagonist activity, and anticonvulsant action of 1-aminocyclobutanecarboxylic acid derivatives.
AID143072Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]glycine as the radioligand.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID144892Inhibition of [3H]-CGS- 19755 binding to N-methyl-D-aspartic acid receptors in rat crude synaptic membranes1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
AID92947Binding affinity towards AMPA receptor using [3H]AMPA as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID91469Binding affinity towards Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID143309In vitro binding affinity towards N-methyl-D-aspartate glutamate receptor of the glutamate receptor using [3H]CPP as radioligand in rat cerebral cortical membranes.1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID114702Effective dose of the intraperitoneally administered compound causing loss of traction reflex, was tested in N-methyl-D-aspartic acid convulsions model1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
AID144457Ability to displace [3H]CPP from NMDA receptor in rat brain membrane1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists.
AID144339N-methyl-D-aspartate glutamate receptor antagonistic ability of 100 uM of compound was assessed from the ability to displace [3H]CPP29,30 from rat cortical membranes; No data.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID144770Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane using [3H]glutamate as radioligand1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
AID235250Therapeutic index(TI) expressed as ratio of ataxia ED50 to the MES ED50 was determined1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
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.
AID145097Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]-CPP as the radioligand.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID144769Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane by using [3H]glycine as radioligand1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
AID144621Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
AID144331Binding affinity for glutamate-stimulated TCP binding site of N-methyl-D-aspartate glutamate receptor from rat brain by using [3H]TCP as radioligand; Agonist1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
AID144605Compound tested for affinity towards N-methyl-D-aspartate glutamate receptor by measuring their ability to displace [3H]TCP from rat brain1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
AID114705Effective dose of the intraperitoneally administered compound protecting mice against tonic seizures, was tested in N-methyl-D-aspartic acid convulsions model1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
AID144460Affinity for the NMDA receptor site was assessed by its ability to displace [3H]TCP from its binding site in rat brain2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID144907Inhibitory activity evaluated by its ability to displace [3H]CPP from rat cortical membrane receptor at 10E-5 concentration of the compound1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
AID115599Ability to protect against NMDA-induced lethality in mice after intraperitoneal administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.
AID144911N-methyl-D-aspartate glutamate receptor antagonistic activity was assessed from the ability to displace [3H]CPP29,30 from rat cortical membranes.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID144889Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane was determined by [3H]-CGP- 39653 as radioligand1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
AID113899Maximal electroshock results in mice by iv administration of 3 mg/kg expressed as 50% effective dose1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
AID112373Tested in vivo for inhibition of NMDA induced lethality, in male Swiss-Albino mice after ip administration.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID132435Functional NMDA antagonist activity was confirmed in vivo in mice (intraperitoneally) using an NMDA-induced lethality assay2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID180480Percent inhibition of glutamate activity against cGMP was determined1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID145098Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]TCP as the radioligand.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID196560In vitro antagonist activity by its ability to inhibit glutamate-induced accumulation of [45Ca2+]- in cultured rat cortical neurons.1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
AID144970Inhibition against NMDA receptor by displacement of [3H]TCP binding from rat cortical membranes1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis, resolution, and SAR of (+/-)-2-amino-N-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine++ + and related analogs as noncompetitive NMDA antagonists with neuroprotective properties.
AID144055Compound was evaluated for the inhibition of the binding of [3H]CPP against N-methyl-D-aspartate glutamate receptor in mice1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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 (737)

TimeframeStudies, This Drug (%)All Drugs %
pre-199082 (11.13)18.7374
1990's410 (55.63)18.2507
2000's165 (22.39)29.6817
2010's75 (10.18)24.3611
2020's5 (0.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.28

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 Index8.28 (24.57)
Research Supply Index6.63 (2.92)
Research Growth Index4.91 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (0.26%)5.53%
Reviews1 (0.13%)6.00%
Case Studies2 (0.26%)4.05%
Observational0 (0.00%)0.25%
Other750 (99.34%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]