Page last updated: 2024-11-13

l 701324

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Description

L 701324: a glycine/NMDA receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54682505
CHEMBL ID31741
CHEBI ID92140
SCHEMBL ID1998890
MeSH IDM0249335

Synonyms (59)

Synonym
MLS002153302
bdbm50038168
7-chloro-4-hydroxy-3-(3-phenoxy-phenyl)-1h-quinolin-2-one
7-chloro-4-hydroxy-3-(3-phenoxyphenyl)quinolin-2(1h)-one
HMS3267A09
BRD-K08109516-001-01-1
BIOMOL-NT_000206
l-701,324, >=98% (hplc), solid
NCGC00024864-01
tocris-0907
BPBIO1_001264
smr000326934
l-701,324
MLS000860076
NCGC00024864-02
l 701,324
l-701324
7-chloro-4-hydroxy-3-(3-phenoxy)phenyl-2(1h)-quinolone
2(1h)-quinolinone, 7-chloro-4-hydroxy-3-(3-pheoxyphenyl)-
7-chloro-4-hydroxy-3-(3-pheoxyphenyl)-2(1h)-quinolinone
l 701324
CHEMBL31741 ,
AKOS005067008
7-chloro-2-hydroxy-3-(3-phenoxyphenyl)-1h-quinolin-4-one
2(1h)-quinolinone, 7-chloro-4-hydroxy-3-(3-phenoxyphenyl)-
unii-i9wy146163
142326-59-8
i9wy146163 ,
HMS2234A14
FT-0687292
HMS3370N04
7-chloro-2-hydroxy-3-(3-phenoxyphenyl)-1,4-dihydroquinolin-4-one
l701324
compund 13 [pmid: 8182696]
gtpl4240
SCHEMBL1998890
CS-4968
7-chloro-4-hydroxy-3-(3-phenoxy)phenyl-2(1h)-quinolinone
HY-18698
DTXSID00162016
7-chloro-4-hydroxy-3-(3-phenoxyphenyl)-2(1h)-quinolinone
AKOS026750257
EX-A587
SR-01000597439-1
sr-01000597439
CHEBI:92140
J-007638
l-701
HMS3675F12
BS-15536
Q27078407
BCP14852
HMS3411F12
AMY19321
BRD-K08109516-001-02-9
7-chloro-4-hydroxy-3-(3-phenoxyphenyl)-1h-quinolin-2-one
D70984
A856966
AC-35896

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"In this study, the anticonvulsant and adverse effects of compounds that belong to four different categories of systemically available N-methyl-D-aspartate (NMDA) receptor ligands were compared, namely the competitive antagonist CGP 40116, the noncompetitive antagonist MK-801 (dizocilpine), the glycineB receptor antagonist L-701,324, and the glycineB receptor high-efficacy partial agonist D-cycloserine."( Anti-convulsant and adverse effects of the glycineB receptor ligands, D-cycloserine and L-701,324: comparison with competitive and non-competitive N-methyl-D-aspartate receptor antagonists.
Wlaź, P, 1998
)
0.3

Compound-Compound Interactions

ExcerptReferenceRelevance
" When eliprodil was combined with an ineffective dose of L-701,324 (2."( Anticonvulsant effects of eliprodil alone or combined with the glycineB receptor antagonist L-701,324 or the competitive NMDA antagonist CGP 40116 in the amygdala kindling model in rats.
Ebert, U; Löscher, W; Wlaź, P, 1999
)
0.3
") administration of D-serine, a selective agonist for the glycine site of the NMDA receptors, alone or in combination with morphine using the tail-flick test."( Activation of supraspinal NMDA receptors by both D-serine alone or in combination with morphine leads to the potentiation of antinociception in tail-flick test of rats.
Akahori, K; Hashimoto, A; Ito, K; Jin, XL; Kobayashi, H; Maeda, M; Matsuda, M; Oka, T; Suzuki, T; Takahashi, S; Yoshikawa, M, 2007
)
0.34

Dosage Studied

ExcerptRelevanceReference
" Combination tests of glycineB ligands demonstrated that injection of a fixed dose of ACPC (200 mg/kg) or L-701,324 (3 mg/kg) together with different doses of AMPH or COC practically did not modify dose-response curves of the psychostimulants, nor did it affect their ED50 values."( Lack of effects of glycineB receptor ligands on the psychostimulant-induced discriminative stimuli in rats.
Filip, M; Papp, M; Przegaliński, E, 2000
)
0.31
" Each molecule was screened in at least seven concentrations, such that dose-response curves were obtained for all molecules in the library."( A high-throughput screen for aggregation-based inhibition in a large compound library.
Austin, CP; Babaoglu, K; Feng, BY; Inglese, J; Jadhav, A; Shoichet, BK; Simeonov, A, 2007
)
0.34
" A low dosage of phenobarbital caused a significant increase of the generalized seizure threshold in the L-701,324 pre-treated group, whereas it did not exert a comparable effect in animals that received vehicle during the massive kindling phase."( Pre-treatment with the NMDA receptor glycine-binding site antagonist L-701,324 improves pharmacosensitivity in a mouse kindling model.
Aronica, E; Gorter, J; Potschka, H; Salvamoser, JD; Soerensen, J; van Vliet, EA; Zellinger, C, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
[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 (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
Chain A, CruzipainTrypanosoma cruziPotency3.16230.002014.677939.8107AID1476
TDP1 proteinHomo sapiens (human)Potency19.34750.000811.382244.6684AID686978; AID686979
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency6.30960.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency31.62280.00255.840031.6228AID899
DNA polymerase kappa isoform 1Homo sapiens (human)Potency37.68580.031622.3146100.0000AID588579
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.48130.251215.843239.8107AID504327
[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)
Beta-lactamaseEscherichia coli K-12IC50 (µMol)74.00000.01502.46578.0000AID286782; AID286783
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.00650.00071.600310.0000AID143068; AID143473; AID143608; AID143786; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)0.00570.00071.630610.0000AID143473; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.00880.00061.525710.0000AID143473; AID143786; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)0.00570.00071.747210.0000AID143473; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)0.00570.00071.741110.0000AID143473; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)0.00570.00071.741110.0000AID143473; AID145260; AID242732
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)0.00570.00071.741110.0000AID143473; AID145260; AID242732
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kb0.02800.02800.45400.8800AID196564
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kb0.02800.01180.30660.8800AID196564
Vasopressin V1a receptorRattus norvegicus (Norway rat)Kb0.02800.02800.45400.8800AID196564
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Kb0.02800.02800.45400.8800AID196564
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kb0.02800.00592.09697.0000AID143250; AID196564
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kb0.02800.00040.30280.8800AID196564
Vasopressin V1b receptorRattus norvegicus (Norway rat)Kb0.02800.02800.45400.8800AID196564
Vasopressin V2 receptor Rattus norvegicus (Norway rat)Kb0.02800.02800.45400.8800AID196564
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kb0.02800.00592.41137.0000AID143250; AID196564
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (2)

Processvia Protein(s)Taxonomy
antibiotic catabolic processBeta-lactamaseEscherichia coli K-12
response to antibioticBeta-lactamaseEscherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
beta-lactamase activityBeta-lactamaseEscherichia coli K-12
hydrolase activityBeta-lactamaseEscherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
outer membrane-bounded periplasmic spaceBeta-lactamaseEscherichia coli K-12
periplasmic spaceBeta-lactamaseEscherichia coli K-12
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 (55)

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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID242732In vitro inhibitory concentration against binding of the [3H]glycine to strychnine-insensitive glycine binding sites of rat N-methyl-D-aspartate glutamate receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID286782Aggregate based-inhibition of Escherichia coli AmpC beta lactamase using stringent assay conditions in presence of 0.01% Triton X-100 detergent2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
A high-throughput screen for aggregation-based inhibition in a large compound library.
AID246987In vivo effective dose to protect the mouse (DBA/2J) from audiogenic seizures upon intraperitoneal administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID113804Anticonvulsant activity measured by its ability to protect against audiogenic seizure in DBA/2 mice when dosed intraperitoneally 30 min prior to seizure induction.1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID246996In vivo effective dose against harmaline induced cGMP elevation in mouse cerebellum upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID203505Human serum albumin index was measured by retention time on an HPLC column containing human albumin1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID145260In vitro inhibition of [3H]glycine at NMDA receptor1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID16092Clearance into cortex from rat plasma or PBS1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID143771Inhibition of [3H]glycine to glycine binding site, associated with the N-methyl-D-aspartate glutamate receptor 1 in crude synaptic membranes prepared from adult rat cerebral cortex.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
AID131550Protection from audiogenic seizure in the DBA/2 mouse 30 min after oral administration1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
AID248671In vitro inhibitory concentration against glutamate stimulated accumulation of cyclic GMP in neonatal rat cerebral slices2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID112401compound was evaluated in vivo for their ability to protect against audiogenic seizure in DBA/2 mice when dosed ip 30 min prior to noise stimulation and it is evaluated as ED50 value1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
AID143786Antagonistic activity for suppression of membrane current response elicited by fixed concentration of glycine and glutamate in Xenopus oocyte expressing N-methyl-D-aspartate glutamate receptor 1/2B1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.
AID143250In vitro inhibition of cortical slice at NMDA receptor1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID259813Protection of mice against maximal e-shock at 0.7 mg/kg2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID226499Protein binding index(PBI) reflects the relative displacement of [3H]glycine from rat cortical membranes in the presence and absence of 0.2% human serum albumin1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID259803Effect on plasma tissue level after 6 min at 5 mg/kg, iv2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID246999In vivo effective dose to protect rats against maximal electroshock induced seizures upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID143068Inhibition of the binding of [3H]L-689,560 ([3H]-4) to the strychnine-insensitive glycine site on rat brain membranes1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
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.
AID259804Effect on brain tissue level after 6 min at 5 mg/kg, iv2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID112663In vivo antagonist activity against seizures elicited by audiogenic, administered perorally in mice1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID143473Affinity for the glycine binding site on rat N-methyl-D-aspartate glutamate receptor 1, determined by displacement of the glycine site antagonist [3H]L-689,560 from rat cortical membranes1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID131549Protection from audiogenic seizure in the DBA/2 mouse 30 min after intraperitoneal administration1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
AID112662In vivo antagonist activity against seizures elicited by audiogenic, administered intra peritoneally in mice1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID259805Effect on plasma tissue level after 1h at 5 mg/kg, iv2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID19623Partition coefficient (logP)1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID259801Inhibition of [3H]glycine binding to NMDA receptor in rat brain membranes2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID143610Inhibition of binding of [3H]glycine to N-methyl-D-aspartate glutamate receptor 1 from crude synaptic membranes prepared from adult rat cerebral cortex.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.
AID110057Ability of intravenously administered compound to prevent seizures, induced by NMDLA (500 mg/kg sc) in mice, in the presence of 100 mg/kg of warfarin1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID186995Blockade of NMDA-induced depolarizations on rat cortical slices1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
AID110056Ability of intravenously administered compound to prevent seizures, induced by NMDLA (500 mg/kg sc) in mice1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID286783Inhibition of Escherichia coli AmpC beta lactamase using relaxed assay conditions in presence of 0.00001% Triton X-100 detergent2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
A high-throughput screen for aggregation-based inhibition in a large compound library.
AID259806Effect on brain tissue level after 1h at 5 mg/kg, iv2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
AID110058Ability of intravenously administered compound to prevent seizures, induced by NMDLA (500 mg/kg sc) in mice, in the presence of 60 mg/kg of warfarin1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID143304Displacement of [3H]-5-7 dichlorokynurenic acid ([3H]- DCKA) from N-methyl-D-aspartate glutamate receptor glycine site of rat brain membrane homogenate1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.
AID114334Effective dose to inhibit convulsions induced by NMDA in mice, when administered intravenous route.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
AID143608In vitro ability to displace [3H]L-689,560 binding to glycine site on the N-methyl-D-aspartate (NMDA) glutamate receptor 1 from rat cortical membranes1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
AID246981In vivo effective dose of compound to protect mice from quinolinic acid seizures upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID196564Evaluated to antagonize NMDA responses in a rat cortical slice preparations1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1346641Rat GluN1 (Ionotropic glutamate receptors)1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
AID493017Wombat Data for BeliefDocking1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (70)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's32 (45.71)18.2507
2000's22 (31.43)29.6817
2010's11 (15.71)24.3611
2020's5 (7.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.19

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 Index15.19 (24.57)
Research Supply Index4.39 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.19)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (2.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other78 (97.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]