Page last updated: 2024-12-08

mdl29,951

Cross-References

ID SourceID
PubMed CID446916
CHEMBL ID31344
SCHEMBL ID8463078
MeSH IDM000594717

Synonyms (34)

Synonym
BRD-K59753853-001-01-5
IDI1_018404
BPBIO1_001266
OPREA1_596892
BIOMOL-NT_000207
1LEV
DB04175
3-(2-carboxy-ethyl)-4,6-dichloro-1h-indole-2-carboxylic acid
mdl-29951
NCGC00163269-01
MAYBRIDGE3_007017
HMS1450O21
mdl 29951
CHEMBL31344 ,
3-(2-carboxyethyl)-4,6-dichloro-1h-indole-2-carboxylic acid
bdbm50004952
CS-1958
HY-16312
130798-51-5
2-carboxy-4,6-dichloro-1h-indole-3-propanoic acid
SCHEMBL8463078
AC-35287
HMS3604I17
AKOS026750250
EX-A270
CCG-251602
AS-68689
1h-indole-3-propanoic acid, 2-carboxy-4,6-dichloro-
mfcd00897722
NCGC00163269-02
FT-0700161
Q27095008
BCP08592
A13729

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (21)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Fructose-1,6-bisphosphataseSus scrofa (pig)IC50 (µMol)2.50002.50002.50002.5000AID977608
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC50 (µMol)2.16670.01002.00979.8000AID1076089; AID1076090; AID1189736
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)273.00000.00011.617910.0000AID92506
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)273.00000.00011.700010.0000AID92506
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)273.00000.00011.700010.0000AID92506
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)273.00000.00011.700010.0000AID92506
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC50 (µMol)418.00000.00700.98217.0000AID93726
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)89.59480.00071.600310.0000AID1385402; AID1385403; AID143068; AID145260
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC50 (µMol)418.00000.00701.01327.0000AID93726
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC50 (µMol)418.00000.00701.01327.0000AID93726
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)119.43670.00071.630610.0000AID1385402; AID1385403; AID145260
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)119.43670.00061.525710.0000AID1385402; AID1385403; AID145260
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)90.25250.00071.747210.0000AID1385402; AID1385403; AID143231; AID145260
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC50 (µMol)418.00000.00701.01327.0000AID93726
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)Ki1.99331.21003.03506.5400AID1137663; AID1137664; AID1385418
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)119.43670.00071.741110.0000AID1385402; AID1385403; AID145260
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC50 (µMol)418.00000.00701.01327.0000AID93726
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)119.43670.00071.741110.0000AID1385402; AID1385403; AID145260
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)119.43670.00071.741110.0000AID1385402; AID1385403; AID145260
[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)
Uracil nucleotide/cysteinyl leukotriene receptorRattus norvegicus (Norway rat)EC50 (µMol)0.70500.70500.70500.7050AID1385405
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)EC50 (µMol)0.40960.00630.40960.8128AID1339654; AID1339655
Uracil nucleotide/cysteinyl leukotriene receptorMus musculus (house mouse)EC50 (µMol)1.11001.11001.11001.1100AID1385406
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIFructose-1,6-bisphosphatase 1Homo sapiens (human)
fructose 6-phosphate metabolic processFructose-1,6-bisphosphatase 1Homo sapiens (human)
gluconeogenesisFructose-1,6-bisphosphatase 1Homo sapiens (human)
regulation of gluconeogenesisFructose-1,6-bisphosphatase 1Homo sapiens (human)
dephosphorylationFructose-1,6-bisphosphatase 1Homo sapiens (human)
negative regulation of cell growthFructose-1,6-bisphosphatase 1Homo sapiens (human)
response to nutrient levelsFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to insulin stimulusFructose-1,6-bisphosphatase 1Homo sapiens (human)
negative regulation of glycolytic processFructose-1,6-bisphosphatase 1Homo sapiens (human)
negative regulation of Ras protein signal transductionFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to magnesium ionFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to cAMPFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to xenobiotic stimulusFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular hyperosmotic salinity responseFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular hypotonic salinity responseFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to raffinoseFructose-1,6-bisphosphatase 1Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateFructose-1,6-bisphosphatase 1Homo sapiens (human)
fructose 1,6-bisphosphate metabolic processFructose-1,6-bisphosphatase 1Homo sapiens (human)
fructose metabolic processFructose-1,6-bisphosphatase 1Homo sapiens (human)
sucrose biosynthetic processFructose-1,6-bisphosphatase 1Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
oligodendrocyte differentiationUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
chemokine-mediated signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
positive regulation of Rho protein signal transductionUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
AMP bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
fructose 1,6-bisphosphate 1-phosphatase activityFructose-1,6-bisphosphatase 1Homo sapiens (human)
identical protein bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
metal ion bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
monosaccharide bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingFructose-1,6-bisphosphatase 1Homo sapiens (human)
chemokine receptor activityUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
receptor serine/threonine kinase bindingUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
G protein-coupled receptor activityUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleusFructose-1,6-bisphosphatase 1Homo sapiens (human)
cytoplasmFructose-1,6-bisphosphatase 1Homo sapiens (human)
cytosolFructose-1,6-bisphosphatase 1Homo sapiens (human)
extracellular exosomeFructose-1,6-bisphosphatase 1Homo sapiens (human)
cytoplasmFructose-1,6-bisphosphatase 1Homo sapiens (human)
cytosolFructose-1,6-bisphosphatase 1Homo sapiens (human)
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)
plasma membraneUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
plasma membraneUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
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 (54)

Assay IDTitleYearJournalArticle
AID132457The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intracerebroventricular), for 5 min drug pretreatment time1992Journal 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.
AID1137663Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assay2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
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.
AID1385406Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID71953Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in porcine kidney2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
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.
AID1385417Selectivity ratio of EC50 for mouse GPR17 expressed in HEK293 cells to EC50 for human GPR17 expressed in human 1321N1 cells2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID71952Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in human liver2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
AID132459The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intravenous), for 5 min drug pretreatment time1992Journal 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.
AID1385405Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
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.
AID684832Inhibition of human recombinant FBPase using fructose-1,6-biphosphate as substrate incubated for 3 mins prior to substrate addition by spectrophotometric analysis2012European journal of medicinal chemistry, Oct, Volume: 56Ligand-based designing, in silico screening, and biological evaluation of new potent fructose-1,6-bisphosphatase (FBPase) inhibitors.
AID1385416Selectivity ratio of EC50 for rat GPR17 expressed in HEK293 cells to EC50 for human GPR17 expressed in human 1321N1 cells2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1385403Displacement of [3H]CCP from NMDA receptor glutamate binding site in rat cortical and hippocampal membranes2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1385413Agonist activity at human P2Y12 receptor transfected in CHO cells assessed as induction of beta-arrestin translocation2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1137662Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes assessed as dissociation half life at 100 uM treated after 1 hr incubation with radioligand by liquid scintillation counting2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
AID1385411Agonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UTP by fluo-4 dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1137661Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes assessed as association half life at 100 uM by liquid scintillation counting2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
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.
AID1385402Displacement of [3H]glycine from NMDA receptor in rat cortical and hippocampal membranes2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID132458The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intraperitoneal), for 2 hr drug pretreatment time1992Journal 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.
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.
AID92506The compound was evaluated in vivo for the competitive binding against [3H]-Ionotropic glutamate receptor AMPA 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.
AID1385409Agonist activity at human P2Y1 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of ADP by fluo-4 dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
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.
AID143231Compound was evaluated for in vitro inhibition of cGMP cerebellar slice at NMDA receptor.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID1137664Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
AID71955Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in rabbit liver2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
AID1076089Inhibition of human recombinant FBPase expressed in Escherichia coli BL21(DE3) by phosphoglucose isomerase and glucose-6-phosphate dehydrogenase coupled assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Design, synthesis and biological evaluation of 7-nitro-1H-indole-2-carboxylic acid derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.
AID1189736Inhibition of human liver FBPase expressed in Escherichia coli BL21(DE3) Rosetta cells assessed as reduction of NADP+ to NADPH by phosphoglucose isomerase and glucose-6-phosphate dehydrogenase coupling based spectrophotometry2015European journal of medicinal chemistry, Jan-27, Volume: 90Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.
AID1385412Agonist activity at human P2Y6 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UDP by fluo-4 dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
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.
AID112660In vivo antagonist activity against seizures elicited by audiogenic administered icv in mice1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
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.
AID1385414Agonist activity at human P2Y14 receptor transfected in CHO cells assessed as induction of beta-arrestin translocation2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1385418Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
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.
AID1385410Agonist activity at human P2Y2 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UTP by fluo-4 dye based assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID132456The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid + probenecid seizure model (intravenous), for 5 min drug pretreatment time1992Journal 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.
AID132454The compound was evaluated in vivo for the anticonvulsant activity in audiogenic seizure model (intraperitoneal), for 2 hr drug pretreatment time1992Journal 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.
AID71956Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in rat liver2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
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.
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.
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.
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.
AID93726The compound was evaluated in vivo for the competitive binding against [3H]kainate 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.
AID1076090Inhibition of FBPase (unknown origin)2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Design, synthesis and biological evaluation of 7-nitro-1H-indole-2-carboxylic acid derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.
AID1347160Primary screen NINDS Rhodamine 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine 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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (33.33)18.2507
2000's1 (6.67)29.6817
2010's7 (46.67)24.3611
2020's2 (13.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (93.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
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