Page last updated: 2024-11-12

alx 1393

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

Description

ALX 1393: a GlyT2 inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16078939
CHEMBL ID475562
MeSH IDM0534684

Synonyms (18)

Synonym
alx-1393, >98% (hplc), powder
NCGC00165720-01
(2s)-2-amino-3-((2-(benzyloxy)phenyl)(3-fluorophenyl)methoxy)propanoic acid
bdbm50256745
CHEMBL475562 ,
alx-1393
o-[(2-benzyloxyphenyl-3-flurophenyl)methyl]-l-serine
alx 1393
gtpl4622
o-[2-benzyloxyphenyl-3-flurophenyl]methyl-l-serine
alx1393
(2s)-2-amino-3-{[2-(benzyloxy)phenyl](3-fluorophenyl)methoxy}propanoic acid
HY-111029
Q27074419
949164-09-4
(2s)-2-amino-3-[(3-fluorophenyl)-(2-phenylmethoxyphenyl)methoxy]propanoic acid
CS-0033998
AKOS040741096
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Galanin receptor type 2Rattus norvegicus (Norway rat)IC50 (µMol)0.02110.02110.02110.0211AID367019
Sodium- and chloride-dependent glycine transporter 1Homo sapiens (human)IC50 (µMol)4.00000.000412.2769106.0000AID1388339
Sodium- and chloride-dependent glycine transporter 2Homo sapiens (human)IC50 (µMol)0.07530.026012.7472128.0000AID1388338; AID1634027; AID1638513
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
negative regulation of NMDA glutamate receptor activitySodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
neurotransmitter transportSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
glycine transportSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
positive regulation of hemoglobin biosynthetic processSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
regulation of synaptic transmission, glycinergicSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
positive regulation of heme biosynthetic processSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
glycine import across plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
synaptic transmission, glycinergicSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
neurotransmitter transportSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
chemical synaptic transmissionSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
synaptic transmission, glycinergicSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
glycine import across plasma membraneSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
glycine transmembrane transporter activitySodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
glycine:sodium symporter activitySodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
glycine:sodium symporter activitySodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
metal ion bindingSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
endosomeSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
basal plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
postsynaptic densitySodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
apical plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
lateral plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
synaptic vesicle membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
dense core granuleSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
parallel fiber to Purkinje cell synapseSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent glycine transporter 1Homo sapiens (human)
endosomeSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
plasma membraneSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
membraneSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
dense core granuleSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
glycinergic synapseSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
plasma membraneSodium- and chloride-dependent glycine transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1388341Unbound brain to plasma concentration ratio in mouse2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1634027Inhibition of human GlyT2 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake at pH 7.5 by scintillation spectroscopy2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations.
AID367018Inhibition of [3H]glycine uptake at rat glycine transporter 1 expressed in african green monkey COS7 cells2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1).
AID1638513Inhibition of full length human GlyT2 expressed in FreeStyle 293-F suspension cells incubated for 30 mins before [3H]glycine addition and measured after 30 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain.
AID1388339Inhibition of human GlyT-1 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake preincubated for 30 mins followed by 3H]-glycine addition measured after 30 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388338Inhibition of human GlyT-2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake preincubated for 30 mins followed by 3H]-glycine addition measured after 30 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388346Antiallodynic activity in spinal cord injury Sprague-Dawley rat model assessed as inhibition of non-voiding contraction amplitude at 10 ug, it relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388347Antiallodynic activity in spinal cord injury Sprague-Dawley rat model assessed as inhibition of non-voiding contraction frequency at 10 ug, it relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388349Antiallodynic activity in spinal cord injury Sprague-Dawley rat model assessed as inhibition of non-voiding contraction frequency at 30 ug, it relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388348Antiallodynic activity in spinal cord injury Sprague-Dawley rat model assessed as inhibition of non-voiding contraction amplitude at 30 ug, it relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID1388340Selectivity ratio of IC50 for human GlyT-1 expressed in HEK293 cells to IC50 for human GlyT-2 expressed in HEK293 cells2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID367020Inhibition of [3H]glycine uptake in human T98G cells2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1).
AID367019Inhibition of [3H]glycine uptake at rat glycine transporter 2 expressed in african green monkey COS7 cells2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (11.11)29.6817
2010's15 (83.33)24.3611
2020's1 (5.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.07

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 Index17.07 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]