Page last updated: 2024-12-11

alx 5407

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

Cross-References

ID SourceID
PubMed CID6604909
CHEMBL ID180966
CHEBI ID92943
SCHEMBL ID1052569
MeSH IDM0498154

Synonyms (24)

Synonym
{[(r)-3-(biphenyl-4-yloxy)-3-(4-fluoro-phenyl)-propyl]-methyl-amino}-acetic acid
bdbm50149871
(r)-2-((3-(biphenyl-4-yloxy)-3-(4-fluorophenyl)propyl)(methyl)amino)acetic acid
BRD-K53979406-003-01-0
tocris-1757
NCGC00025278-01
alx-5407
CHEMBL180966 ,
2-[[(3r)-3-(4-fluorophenyl)-3-(4-phenylphenoxy)propyl]-methylamino]acetic acid
(r)-nfps
(+)-nfps
alx 5407
gtpl4618
2-{[(3r)-3-(4-fluorophenyl)-3-(4-phenylphenoxy)propyl](methyl)amino}acetic acid
SCHEMBL1052569
571147-18-7
SR-01000597496-1
sr-01000597496
CHEBI:92943
(r)-(n-[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy)propyl])sarcosine
(r)-n-(3-([1,1'-biphenyl]-4-yloxy)-3-(4-fluorophenyl)propyl)-n-methylglycine
Q27088566
NCGC00025278-02
DTXSID401025863
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[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 (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency19.95260.002014.677939.8107AID1476
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency12.58930.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency44.66840.011212.4002100.0000AID1030
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency6.30960.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency2.51190.00636.904339.8107AID883
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency2.51190.00638.235039.8107AID883
[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)
Sodium- and chloride-dependent glycine transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00460.00040.00460.0089AID639652; AID768449
Sodium- and chloride-dependent glycine transporter 1Homo sapiens (human)IC50 (µMol)0.00930.000412.2769106.0000AID1388362; AID1559416; AID1634028; AID241454; AID639652
Galanin receptor type 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00300.00300.00300.0030AID367018
Sodium- and chloride-dependent glycine transporter 2Homo sapiens (human)IC50 (µMol)15.90000.026012.7472128.0000AID1634027; AID308947
[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 (17)

Assay IDTitleYearJournalArticle
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.
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).
AID308947Inhibition of [14C]glycine reuptake at human GlyT2 expressed in BE(2)-C cells2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Discovery and SAR studies of novel GlyT1 inhibitors.
AID1634028Inhibition of human GlyT1 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake incubated for 10 mins at pH 7.4 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.
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).
AID1388362Inhibition of human GlyT-12018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
AID639652Inhibition of GlyT1 in human JAR cells assessed as inhibition of [3H]glycine uptake preincubated for 1 mins measured after 2 hrs by liquid scintillation counting2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Synthesis and characterization of [¹²⁵I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1.
AID1629932Competitive inhibition of glycine transporter-1 (unknown origin) expressed in HEK293 cells at 0.62 to 17 nM in presence of [3H]glycine by scintillation proximity assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.
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).
AID1634029Inhibition of human GlyT1 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake incubated for 10 mins at pH 7.4 by scintillation spectroscopy relative to untreated control2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations.
AID1559416Inhibition of human GlyT1 expressed in QT6 cells assessed as reduction in [14C]glycine uptake incubated for 20 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
The Druggability of Solute Carriers.
AID768449Displacement of [3H]glycine from GlyT1 in rat C6 glioma cells incubated for 30 mins prior to substrate addition measured after 10 mins by scintillation counting analysis2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Atropisomeric 4-phenyl-4H-1,2,4-triazoles as selective glycine transporter 1 inhibitors.
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.
AID241454Inhibition of uptake of [3H]-glycine into cells transfected with human GlyT-1b transporter2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.
AID308948Increase in glycine level of Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, sc2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Discovery and SAR studies of novel GlyT1 inhibitors.
AID308949Drug level in rat cerebrospinal fluid at 30 mg/kg, sc2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Discovery and SAR studies of novel GlyT1 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (27.27)29.6817
2010's5 (45.45)24.3611
2020's3 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.72

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 Index24.72 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.84 (4.65)
Search Engine Demand Index17.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (18.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (81.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]