Page last updated: 2024-12-08

d-apv

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

Cross-References

ID SourceID
PubMed CID135342
CHEMBL ID84612
SCHEMBL ID158653
MeSH IDM0024151

Synonyms (61)

Synonym
CHEMBL84612
d-apv
PDSP1_000129
NCGC00024470-01
NCGC00015065-01
lopac-a-5282
tocris-0106
tocris-0105
NCGC00024471-01
PDSP2_000128
d(-)-2-amino-5-phosphonopentanoic acid, nmda receptor antagonist
d-(-)-2-amino-5-phosphonopentanoic acid
d-ap5
d-norvaline, 5-phosphono-
5-phosphono-d-norvaline
d-2-amino-5-phosphopentanoic acid
(r)-2-amino-5-phosphonopentanoic acid ,
79055-68-8
(2r)-2-amino-5-phosphonopentanoic acid
cas_79055-68-8
cb3371309
bdbm81977
HMS3261C18
AKOS006274118
NCGC00015065-02
d(-)-2-amino-5-phosphonovaleric acid (d-ap5)
d(-)-2-amino-5-phosphonopentanoic acid
LP00418
d-2-amino-5-phosphonovaleric acid
CCG-221722
2jj ,
SCHEMBL158653
tox21_500418
NCGC00261103-01
(2r)-amino-5-phosphonovaleric acid
d-2-amino-5-phosphonovalerate
HB0225
mfcd00078839
(r)-(-)-2-amino-5-phosphonopentanoic acid
sr-01000597642
SR-01000597642-3
VOROEQBFPPIACJ-SCSAIBSYSA-N
d-(-)-2-amino-5-phosphonopentanoic acid - cas 79055-68-8
BD162474
Q209309
HY-100714A
CS-0020421
SDCCGSBI-0633711.P001
NCGC00024471-03
(2r)-2-amino-5-phosphonopentanoic acid.
D92988
d-apv;d-2-amino-5-phosphonovaleric acid
DTXSID201000239
d-2-amino-5-phosphonovaleric acidd-apv
d-2-amino-5-phosphonopentanoic acid
EX-A6457
2-amino-5-phosphonovalerate, (r)-
(r)-ap-5
(-)-2-amino-5-phosphonopentanoic acid
CD39X2NL7F
2-amino-5-phosphonopentanoic acid, (r)-
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency24.36160.177814.390939.8107AID2147
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency5.01190.02827.055915.8489AID895; AID928
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.49050.001530.607315,848.9004AID1224819; AID1224820
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.38720.00106.000935.4813AID944
[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 ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.600310.0000AID144763
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki4.63860.00030.86666.6900AID1472311; AID1472312; AID1472313; AID1472314; AID239664; AID239665; AID239666
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.630610.0000AID144763
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.33500.00030.68056.6900AID1472311; AID239664
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.88000.00061.525710.0000AID144763
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki1.63000.00030.70716.6900AID1472312; AID239665
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.747210.0000AID144763
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki3.77000.00030.81966.6900AID1472313; AID239666
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.741110.0000AID144763
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki21.00000.00030.70726.6900AID1472314
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.741110.0000AID144763
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)0.88000.00071.741110.0000AID144763
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
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 (38)

Assay IDTitleYearJournalArticle
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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
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.
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.
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.
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.
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.
AID239721Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2B expressed in Xenopus oocytes compared to NR1a/NR2C2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID146058Effective concentration against NR1/NR2A receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID239722Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2D expressed in Xenopus oocytes compared to NR1a/NR2C2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID239119Displacement of L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure-activity relationships.
AID1472313Antagonist activity at recombinant rat GluN1a/GluN2C expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID1472323Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as LPS-stimulated PGE2 levels at 10 uM after 24 hrs by LC-MS/MS method (Rvb = 162 +/- 7%)2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID146064Effective concentration against NR1/NR2D receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID295004Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid.
AID146062Effective concentration against NR1/NR2C receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID239664Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID1472314Antagonist activity at recombinant rat GluN1a/GluN2D expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID1472350Antiproliferative activity against Nras driven p53 deficient mouse HCC cells assessed as cell viability at 100 uM after 72 hrs by resazurin assay relative to control2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID1472312Antagonist activity at recombinant rat GluN1a/GluN2B expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID1472349Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as potentiation of 10 uM sorafenib-mediated antiproliferative activity by measuring cell viability at 100 uM after 72 hrs by resazurin assay (Rvb = 31 +/- 2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID709976Antagonist activity at NMDA receptor GluN2B subunit in FVB mouse CA1 pyramidal neurons assessed as decrease in EPSC amplitude at holding potential of -60 mV at 50 uM measured at 5 mins by patch clamp electrophysiological assay in presence of Mg2+ free ACS2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Synthesis and biological characterization of 3-substituted 1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors. Part 2.
AID1472346Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as potentiation of 1 uM sorafenib-mediated antiproliferative activity by measuring cell viability at 100 uM after 72 hrs by resazurin assay (Rvb = 88 +/- 32017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID239665Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2B expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID1472333Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as PGE2 levels at 10 uM after 24 hrs by LC-MS/MS method relative to control2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID295005Displacement of [3H]KA from KA receptor in rat cortical membrane2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid.
AID1472348Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as potentiation of 5 uM sorafenib-mediated antiproliferative activity by measuring cell viability at 100 uM after 72 hrs by resazurin assay (Rvb = 72 +/- 12017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID144763In vitro binding affinity for rat cortical membrane N-methyl-D-aspartate glutamate receptor determined using [3H]CPP as radioligand2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID239667Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2D expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID239720Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes compared to NR1a/NR2C2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID1472311Antagonist activity at recombinant rat GluN1a/GluN2A expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID1472332Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as inhibition of NMDA-induced intracellular Ca2+ transients at 20 uM after 48 hrs by fluo-4AM dye-based fluorescence assay2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID239666Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2C expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
AID1472347Antagonist activity at NMDA receptor in Nras driven p53 deficient mouse HCC cell membranes assessed as potentiation of 2.5 uM sorafenib-mediated antiproliferative activity by measuring cell viability at 100 uM after 72 hrs by resazurin assay (Rvb = 82 +/-2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
AID146060Effective concentration against NR1/NR2B receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (35.71)29.6817
2010's5 (35.71)24.3611
2020's4 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.82

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.82 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index5.07 (4.65)
Search Engine Demand Index39.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]