Page last updated: 2024-12-04

5,7-dichlorokynurenic acid

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Description

5,7-dichlorokynurenic acid: potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
GlycinegenusA non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID1779
CHEMBL ID50267
CHEBI ID107660
SCHEMBL ID158714
SCHEMBL ID8369562
MeSH IDM0181715

Synonyms (100)

Synonym
HMS3266E21
BRD-K60287130-001-03-2
gtpl2361
DIVK1C_006856
EU-0100438
SPECTRUM_001455
lopac-d-138
NCGC00015313-01
NCGC00024525-01
tocris-0286
LOPAC0_000438
BIOMOL-NT_000180
BSPBIO_003412
OPREA1_091974
SPECTRUM5_001096
BPBIO1_001172
PDSP1_000183
5,7-dichloro-4-hydroxyquinoline-2-carboxylic acid
5,7 dichlorokynurenic acid
5,7-dichlorokynurenic acid
5,7-dichloroquinurenic acid
5,7-dcka
1PBQ ,
5,7-dichorokynurenic acid
DB01931
NCGC00024525-05
NCGC00024525-03
5,7-dichloro-4-hydroxy-2-quinolinecarboxylic acid
2-quinolinecarboxylic acid, 5,7-dichloro-4-hydroxy-
KBIO3_002632
KBIO1_001800
KBIO2_007071
KBIO2_004503
KBIOGR_000350
KBIO2_001935
KBIOSS_001935
SPECTRUM4_000085
SPECTRUM2_001999
SPECTRUM3_001736
SPBIO_002217
SPECPLUS_000760
SPECTRUM1502062
PDSP2_000182
NCGC00024525-02
NCGC00024525-06
NCGC00024525-04
NCGC00015313-03
CHEBI:107660
NCGC00015313-08
CHEMBL50267 ,
131123-76-7
5,7-dichloro-4-hydroxy-quinoline-2-carboxylic acid
5,7-dichloro-4-hydroxy-quinoline-2-carboxylic acid(dcka)
5,7-dichloro-4-oxo-1,4-dihydro-quinoline-2-carboxylic acid
bdbm50001266
5,7-dichloro-4-hydroxy-quinoline-2-carboxylic acid anion
5,7-dichloro-4-oxo-1h-quinoline-2-carboxylic acid
HMS3261G18
CCG-39537
NCGC00015313-06
NCGC00015313-04
NCGC00015313-05
NCGC00015313-07
NCGC00015313-02
t61ork73py ,
unii-t61ork73py
AKOS012682248
LP00438
AKOS015913821
2-quinolinecarboxylicacid, 5,7-dichloro-4-hydroxy-
SCHEMBL158714
kynurenic acid, 5,7-dichloro-
SCHEMBL8369562
tox21_500438
NCGC00261123-01
2-quinolinecarboxylicacid,5,7-dichloro-4-hydroxy-
J-005939
sr-01000075445
SR-01000075445-3
SR-01000075445-1
dcka; 5,7-dichlorokynurenic acid
DTXSID80893710
Q5204515
FT-0743570
FT-0739743
HMS3675E03
HMS3411E03
BRD-K60287130-001-04-0
BRD-K60287130-001-05-7
SDCCGSBI-0050423.P003
NCGC00015313-10
5,7-dichlorokynurenic-acid
5,7-dichloro-4-oxo-1h-quinoline-2-carboxylic acid.
SB69445
5,7-dichlorokynurenicacidsodiumsalt
BS-20489
CS-0020477
HY-100834
PD002744
mfcd00083173

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" As in the in vitro experiments, the dose-response curve for the antagonist was shifted rightward in a parallel fashion when D-serine was coinjected."( Activity of 5,7-dichlorokynurenic acid, a potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site.
Baron, BM; Harrison, BL; McDonald, IA; Miller, FP; Palfreyman, MG; Salituro, FG; Schmidt, CJ; Sorensen, SM; White, HS, 1990
)
0.66
" Pretreatment with glycine, an agonist to the glycine/NMDA receptors, shifted the dose-response effect of felbamate to the right (ED50 = 56."( Excitatory amino acid neurotransmission through both NMDA and non-NMDA receptors is involved in the anticonvulsant activity of felbamate in DBA/2 mice.
Aguglia, U; Bertorelli, R; De Sarro, A; De Sarro, G; Ongini, E, 1994
)
0.29
" The time course and dose-response relationships for this effect were examined after treatment with two representative antidepressant drugs (imipramine and citalopram) and electriconvulsive shock (ECS)."( Adaptation of the N-methyl-D-aspartate receptor complex following chronic antidepressant treatments.
Layer, RT; Nowak, G; Paul, IA; Popik, P; Skolnick, P, 1994
)
0.29
[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 (35)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.89130.004023.8416100.0000AID485290
thioredoxin reductaseRattus norvegicus (Norway rat)Potency8.43680.100020.879379.4328AID488772; AID488773; AID588453; AID588456
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency63.09570.141337.9142100.0000AID1490
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency0.08491.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.77810.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.58930.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency39.81070.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency29.33010.001815.663839.8107AID894
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.93000.00106.000935.4813AID943; AID944
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.92441.000010.475628.1838AID1457; AID901
[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)
Chain A, N-methyl-D-aspartate Receptor Subunit 1Rattus norvegicus (Norway rat)Ki0.54000.540082.8533241.0000AID977610
Chain A, N-methyl-D-aspartate Receptor Subunit 1Rattus norvegicus (Norway rat)Ki0.54000.540082.8533241.0000AID977610
Chain A, N-methyl-D-aspartate Receptor Subunit 1Rattus norvegicus (Norway rat)Ki0.54000.540082.8533241.0000AID977610
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)75.00000.00011.617910.0000AID92493
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki38.00000.00000.41052.7800AID92652; AID92781
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)75.00000.00011.700010.0000AID92493
Glutamate receptor 2Rattus norvegicus (Norway rat)Ki38.00000.00000.68536.3000AID92652; AID92781
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)75.00000.00011.700010.0000AID92493
Glutamate receptor 3Rattus norvegicus (Norway rat)Ki38.00000.00000.71777.4000AID92652; AID92781
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)75.00000.00011.700010.0000AID92493
Glutamate receptor 4Rattus norvegicus (Norway rat)Ki38.00000.00000.52773.5700AID92652; AID92781
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00700.98217.0000AID93717
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)28.77340.00071.600310.0000AID143167; AID143473; AID143612; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.72570.00030.86666.6900AID143084; AID143299; AID143303; AID143631; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00701.01327.0000AID93717
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00701.01327.0000AID93717
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)40.09280.00071.630610.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki1.22750.00030.68056.6900AID143084; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)40.09280.00061.525710.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki1.22750.00030.70716.6900AID143084; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)40.09280.00071.747210.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki1.22750.00030.81966.6900AID143084; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00701.01327.0000AID93717
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)40.09280.00071.741110.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki1.22750.00030.70726.6900AID143084; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00701.01327.0000AID93717
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)40.09280.00071.741110.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki1.22750.00030.70726.6900AID143084; AID145235; AID145315; AID670582
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)40.09280.00071.741110.0000AID143473; AID144895; AID144896; AID145260
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki1.22750.00030.70726.6900AID143084; AID145235; AID145315; AID670582
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC50 (µMol)0.33000.00301.29038.3000AID143470
TransporterRattus norvegicus (Norway rat)EC50 (µMol)0.33000.00050.04780.3300AID143470
[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)
Glutamate receptor 1Rattus norvegicus (Norway rat)Kb16.50000.59003.33007.0000AID163310; AID187000
Glutamate receptor 2Rattus norvegicus (Norway rat)Kb16.50000.59003.17337.0000AID163310; AID187000
Glutamate receptor 3Rattus norvegicus (Norway rat)Kb16.50000.59003.17787.0000AID163310; AID187000
Glutamate receptor 4Rattus norvegicus (Norway rat)Kb16.50000.59003.28567.0000AID163310; AID187000
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)Kb30.00001.29004.96339.0000AID91453
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kb3.00000.00592.09697.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)Kb30.00001.29004.96339.0000AID91453
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Kb30.00001.29004.04509.0000AID91453
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)Kb30.00001.29004.96339.0000AID91453
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)Kb30.00001.29004.96339.0000AID91453
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kb3.00000.00592.41137.0000AID143250; AID145182; AID187000
[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)
plasma membraneGlutamate receptor 2Rattus 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 (98)

Assay IDTitleYearJournalArticle
AID144468Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]-glycine as the radioligand.1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
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.
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.
AID132519Concentration necessary for 50% inhibition of depolarization induced by 5 uM NMDA in mouse cortical wedge preparation2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID143790Ability to compete with [3H]CCP for rat cortical and hippocampal membrane glutamate binding site.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.
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.
AID163310Apparent dissociation constant of [3H]AMPA from quisqualate receptor of rat cortical slice1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID92493Inhibition of [3H]-AMPA binding to AMPA receptor of rat cortical membrane1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID143163Concentration required to inhibit 50% of the specific binding of [3H]glycine to NMDA receptor prepared from rat cerebral cortex and hippocampus1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.
AID144181Apparent dissociation constant of [3H]glycine from N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation expressed as log values.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID93717Inhibition of [3H]-kainic acid binding to kainate receptor of rat cortical membrane1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID143299Ability to displace strychnine-insensitive [3H]glycine binding to rat cortical membranes.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.
AID92629Percentage inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA of rat cortical membranes at 32 uM2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.
AID132328Ability to inhibit depolarizations induced by NMDA in mouse cortical wedge preparations.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
AID143167Inhibition of [3H]-MK-801 binding to a N-methyl-D-aspartic acid(NMDA) receptor in glycine-sensitive rat cortical membranes.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.
AID93731Inhibition of [3H]KA binding to kainate receptor in rat brain membranes2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
AID143303Displacement of [3H]glycine from glycine site on the NMDA receptor.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.
AID132520Concentration necessary for 50% inhibition of depolarization induced by 5 uM S-AMPA in mouse cortical wedge preparation2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID227647Activity was determined by inhibition of glutamate stimulated accumulation of cyclic GMP in neonatal rat cerebral slices.1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
AID145182Apparent dissociation constant of [3H]glycine from N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID143157Antagonistic activity against N-methyl-D-aspartate glutamate receptor induced cGMP in rat cerebellar slices..1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
AID91446Compound was evaluated for inhibition of binding of [3H]KA to specific binding at Ka receptor in rat cortical membrane at 100 uM2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
AID179379Concentration giving 50% inhibition of stimulated [3H](+)-MK-801 binding in rat cortical membranes incubated with 10 uM glycine2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID670588Antagonist activity at AMPA receptor in mouse cortical wedge assessed as inhibition of S-AMPA-induced membrane depolarization by electrophysiological assay2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
AID143631Binding affinity towards N-methyl-D-aspartate glutamate receptor 1 (high affinity) of rat cortical synaptic membranes by using [3H]Gly as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID113249Antagonist activity in audiogenic seizure model in vivo through icv route1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID112691In vivo anticonvulsant activity determined as icv dose that blocked NMDA-induced tonic seizures induced in DBA/2 mice after ip administration2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID112692In vivo anticonvulsant activity determined as icv dose that blocked clonic seizures induced by audiogenic stimuli in DBA/2 mice after pretreatment with D-serine2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID143084Affinity for the glycine binding site of NMDA receptor by inhibition of [3H]5,7-dichlorokynurenic acid ([3H]DCKA) binding to rat brain synaptic membrane1994Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
Tricyclic quinoxalinediones: 5,6-dihydro-1H-pyrrolo[1,2,3-de] quinoxaline-2,3-diones and 6,7-dihydro-1H,5H-pyrido[1,2,3-de] quinoxaline-2,3-diones as potent antagonists for the glycine binding site of the NMDA receptor.
AID145315Ability to displace [3H]glycine from NMDA receptor in rat corticaln membranes2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
AID144896Inhibition of [3H]glycine binding to glycine site of N-methyl-D-aspartate glutamate receptor in rat cortical membranes1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID114663Separation-induced vocalization in vivo through ip route1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID92652Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.
AID92789Compound was evaluated for inhibition of binding of [3H]AMPA to specific binding at Ionotropic glutamate receptor AMPA in rat cortical membrane at 100 uM2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
AID143618Ability to compete with [3H]glycine for strychnine-insensitive binding sites on rat cortical and hippocampal membrane1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.
AID143470Functional antagonism at the N-methyl-D-aspartate glutamate receptor 1 was demonstarted by the ability to inhibit the binding of the channel-blocking agent [3H](+)-MK-8011999Journal of medicinal chemistry, Jul-01, Volume: 42, Issue:13
4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.
AID112694In vivo anticonvulsant activity determined as icv dose that blocked tonic seizures induced by audiogenic stimuli in DBA/2 mice after pretreatment with D-serine2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID93730Percent inhibition of compound at 100 uM towards high-affinity Ionotropic glutamate receptor kainate of rat cortical membranes by using [3H]KA as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID670587Antagonist activity at NMDA receptor in mouse cortical wedge assessed as inhibition of NMDA-induced membrane depolarization by electrophysiological assay2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
AID144172Antagonism at NMDA receptor in mouse cortical wedge preparation expressed as concentration that inhibits by 50% depolarizations induced by 5 uM AMPA2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
AID112695In vivo anticonvulsant activity determined as icv dose that blocked tonic seizures induced in DBA/2 mice by audiogenic stimuli2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID112689In vivo anticonvulsant activity determined as icv dose that blocked 3,5-DHPG induced tonic seizures induced in DBA/2 mice after2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID143781Activity against rat cortical and hippocampal membrane N-methyl-D-aspartate glutamate receptor 1/2A/2B/2C/2D using [3H]CPP1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
AID143765Selectivity ratio for CPP and gly NMDA binding1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
AID112693In vivo anticonvulsant activity determined as icv dose that blocked clonic seizures induced in DBA/2 mice by audiogenic stimuli2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID92049Antagonism at ionotropic glutamate receptor AMPA in mouse cortical wedge preparation2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
AID92628Percent inhibition of compound at 100 uM concentration towards Ionotropic glutamate receptor AMPA (high-affinity) of rat cortical synaptic membranes by using [3H]AMPA as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
AID143472Activity against rat cortical and hippocampal membrane strychnine-insensitive N-methyl-D-aspartate glutamate receptor 1 using [3H]-gly1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
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.
AID145235Inhibitory concentration of compound for depolarization induced by 5 uM NMDA in mouse cortical wedge preparation2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
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.
AID670585Displacement of [3H]kainate from kainate receptor in rat cortical membrane at 100 uM2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
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.
AID147190Inhibition of [125I]- NGF binding to extracellular domain of p75 receptor; IA=Inactive1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Kynurenic acid derivatives inhibit the binding of nerve growth factor (NGF) to the low-affinity p75 NGF receptor.
AID144467Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]CPP as the radioligand.1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
AID132325Ability to inhibit depolarizations induced by AMPA in mouse cortical wedge preparations2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
AID670586Displacement of [3H](+)MK-801 from N-methyl D-aspartate receptor in rat cortical membrane2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
AID670581Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptical membrane at 100 uM2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
AID670582Displacement of [3H]glycine from NMDA receptor in rat cortical synaptical membrane2012European journal of medicinal chemistry, Aug, Volume: 543-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
AID234200Ratio of the inhibitory activity against [3H]-CCP for rat cortical and hippocampal membrane glutamate binding site to [3H]glycine for rat cortical and hippocampal membrane binding site.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.
AID112690In vivo anticonvulsant activity determined as icv dose that blocked NMDA-induced clonic seizures induced in DBA/2 mice2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID144895Inhibition of [3H]-glutamate binding to N-methyl-D-aspartate glutamate receptor of rat cortical membranes1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID187000Functional antagonistic potency assessed by determination of the apparent dissociation constant for antagonism of the depolarizations induced by NMDA and AMPA in rat cortical slice preparation1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.
AID143612Inhibition of specific binding of [3H]glycine to NMDA receptors, in rat cortical membranes at 32 uM conc.2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.
AID430787Antagonist activity at glycine site of NMDA receptor in rat brain cortex membrane assessed as inhibition of [3H]Mk-801 binding by liquid scintillation counting in presence of maximally active glycine2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex.
AID91453Apparent dissociation constant of [3H]kainate from Ionotropic glutamate receptor ionotropic kainate was determined in rat cortical slice preparation1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
AID92781Inhibitory concentration of compound for depolarization induced by 5 uM S-AMPA in mouse cortical wedge preparation2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
AID229653Selectivity ratio as the ratio of IC50 values for [3H]CPP/[3H]-gly1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
AID112661In 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.
AID73797Compound was evaluated for inhibition of binding of [3H]glycine to specific binding at glycine receptor in rat cortical membrane2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
AID112688In vivo anticonvulsant activity determined as icv dose that blocked 3,5-DHPG induced clonic seizures induced in DBA/2 mice2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.
AID92513Binding affinity at ionotropic glutamate receptor AMPA in rat cortical membranes using [3H]AMPA radioligand2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
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.
AID179408Concentration that inhibits 50% S-AMPA stimulated (50 uM) [3H]norepinephrine release from rat hippocampal synaptosomes2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2003The EMBO journal, Jun-16, Volume: 22, Issue:12
Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core.
AID1811Experimentally measured binding affinity data derived from PDB2003The EMBO journal, Jun-16, Volume: 22, Issue:12
Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core.
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 (142)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's82 (57.75)18.2507
2000's38 (26.76)29.6817
2010's16 (11.27)24.3611
2020's6 (4.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.44

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 Index14.44 (24.57)
Research Supply Index5.01 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (0.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other148 (99.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]