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 Source | ID |
|---|---|
| PubMed CID | 6604909 |
| CHEMBL ID | 180966 |
| CHEBI ID | 92943 |
| SCHEMBL ID | 1052569 |
| MeSH ID | M0498154 |
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)
| Class | Description |
|---|---|
| biphenyls | Benzenoid 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
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 19.9526 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| TDP1 protein | Homo sapiens (human) | Potency | 31.6768 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 12.5893 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 44.6684 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 6.3096 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 2.5119 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 2.5119 | 0.0063 | 8.2350 | 39.8107 | AID883 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Sodium- and chloride-dependent glycine transporter 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0046 | 0.0004 | 0.0046 | 0.0089 | AID639652; AID768449 |
| Sodium- and chloride-dependent glycine transporter 1 | Homo sapiens (human) | IC50 (µMol) | 0.0093 | 0.0004 | 12.2769 | 106.0000 | AID1388362; AID1559416; AID1634028; AID241454; AID639652 |
| Galanin receptor type 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0030 | 0.0030 | 0.0030 | AID367018 |
| Sodium- and chloride-dependent glycine transporter 2 | Homo sapiens (human) | IC50 (µMol) | 15.9000 | 0.0260 | 12.7472 | 128.0000 | AID1634027; AID308947 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (11)
Molecular Functions (3)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| glycine transmembrane transporter activity | Sodium- and chloride-dependent glycine transporter 1 | Homo sapiens (human) |
| glycine:sodium symporter activity | Sodium- and chloride-dependent glycine transporter 1 | Homo sapiens (human) |
| glycine:sodium symporter activity | Sodium- and chloride-dependent glycine transporter 2 | Homo sapiens (human) |
| metal ion binding | Sodium- and chloride-dependent glycine transporter 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (15)
Bioassays (17)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID367018 | Inhibition of [3H]glycine uptake at rat glycine transporter 1 expressed in african green monkey COS7 cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1). |
| AID308947 | Inhibition of [14C]glycine reuptake at human GlyT2 expressed in BE(2)-C cells | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Discovery and SAR studies of novel GlyT1 inhibitors. |
| AID1634028 | Inhibition 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 | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations. |
| AID367020 | Inhibition of [3H]glycine uptake in human T98G cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1). |
| AID1388362 | Inhibition of human GlyT-1 | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain. |
| AID639652 | Inhibition of GlyT1 in human JAR cells assessed as inhibition of [3H]glycine uptake preincubated for 1 mins measured after 2 hrs by liquid scintillation counting | 2011 | Bioorganic & 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. |
| AID1629932 | Competitive 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 assay | 2016 | Journal 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. |
| AID367019 | Inhibition of [3H]glycine uptake at rat glycine transporter 2 expressed in african green monkey COS7 cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1). |
| AID1634029 | Inhibition 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 control | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations. |
| AID1559416 | Inhibition of human GlyT1 expressed in QT6 cells assessed as reduction in [14C]glycine uptake incubated for 20 mins by liquid scintillation counting method | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | The Druggability of Solute Carriers. |
| AID768449 | Displacement 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 analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Atropisomeric 4-phenyl-4H-1,2,4-triazoles as selective glycine transporter 1 inhibitors. |
| AID1634027 | Inhibition of human GlyT2 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake at pH 7.5 by scintillation spectroscopy | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations. |
| AID241454 | Inhibition of uptake of [3H]-glycine into cells transfected with human GlyT-1b transporter | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15 | The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors. |
| AID308948 | Increase in glycine level of Sprague-Dawley rat cerebrospinal fluid at 30 mg/kg, sc | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Discovery and SAR studies of novel GlyT1 inhibitors. |
| AID308949 | Drug level in rat cerebrospinal fluid at 30 mg/kg, sc | 2007 | Bioorganic & 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (27.27) | 29.6817 |
| 2010's | 5 (45.45) | 24.3611 |
| 2020's | 3 (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.
| This Compound (24.72) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (18.18%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (81.82%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||