Page last updated: 2024-11-13
vu0422288
Description
Research Excerpts
Clinical Trials
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Study Profile
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Description
VU0422288: a positive allosteric modulator of metabotropic glutamate receptor 7; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 73058507 |
| CHEMBL ID | 4162576 |
| SCHEMBL ID | 20166019 |
| MeSH ID | M000609042 |
Synonyms (21)
| Synonym |
|---|
| bdbm50283487 |
| chembl4162576 , |
| VU0422288-4 |
| ml 396 |
| 1630936-95-6 |
| vu 0422288 |
| n-[3-chloro-4-[(5-chloro-2-pyridinyl)oxy]phenyl]-2-pyridinecarboxamide |
| AKOS025293496 |
| n-(3-chloro-4-((5-chloropyridin-2-yl)oxy)phenyl)picolinamide |
| ml396, >=98% (hplc) |
| n-[3-chloro-4-(5-chloropyridin-2-yl)oxyphenyl]pyridine-2-carboxamide |
| SCHEMBL20166019 |
| ml-396 |
| gtpl10239 |
| vu0422288 |
| n-{3-chloro-4-[(5-chloropyridin-2-yl)oxy]phenyl}pyridine-2-carboxamide |
| vu-0422288 |
| NCGC00476190-02 |
| MS-25683 |
| HY-110190 |
| CS-0033054 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (4)
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | EC50 (µMol) | 0.1080 | 0.0001 | 0.2328 | 3.2000 | AID1492909 |
| Metabotropic glutamate receptor 7 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1460 | 0.1460 | 0.8230 | 1.5000 | AID1492913; AID1571664 |
| Metabotropic glutamate receptor 8 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1250 | 0.0310 | 1.1813 | 8.0000 | AID1492915; AID1571665 |
| Metabotropic glutamate receptor 4 | Homo sapiens (human) | EC50 (µMol) | 0.1080 | 0.0040 | 1.7193 | 9.8000 | AID1492909; AID1571663 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (26)
Molecular Functions (26)
Ceullar Components (6)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytoplasm | Cytochrome P450 3A4 | Homo sapiens (human) |
| endoplasmic reticulum membrane | Cytochrome P450 3A4 | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Cytochrome P450 3A4 | Homo sapiens (human) |
| plasma membrane | Metabotropic glutamate receptor 4 | Homo sapiens (human) |
| cytoplasmic vesicle | Metabotropic glutamate receptor 4 | Homo sapiens (human) |
| presynapse | Metabotropic glutamate receptor 4 | Homo sapiens (human) |
| plasma membrane | Metabotropic glutamate receptor 4 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (8)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1571664 | Agonist activity at rat mGlu7 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present. |
| AID1571663 | Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present. |
| AID1571665 | Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present. |
| AID1492913 | Positive allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| AID1492915 | Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| AID1492909 | Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye b | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-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 (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 5 (83.33) | 24.3611 |
| 2020's | 1 (16.67) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||