Page last updated: 2024-11-12
ubp296
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
UBP296: potent and selective kainate receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11674376 |
| CHEMBL ID | 372631 |
| CHEBI ID | 91719 |
| SCHEMBL ID | 2265718 |
| MeSH ID | M0472841 |
Synonyms (23)
| Synonym |
|---|
| HMS3268J09 |
| HMS3268J11 |
| CHEMBL372631 , |
| bdbm50178148 |
| (rs)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione |
| ubp 296 |
| BRD-A45499626-001-01-0 |
| SCHEMBL2265718 |
| 745055-86-1 |
| AKOS024456931 |
| SR-01000597532-1 |
| sr-01000597532 |
| CHEBI:91719 |
| 2-[[3-(2-amino-2-carboxyethyl)-2,6-dioxo-1-pyrimidinyl]methyl]benzoic acid |
| Q27163534 |
| HMS3677E09 |
| HMS3413E09 |
| BRD-A45499626-001-02-8 |
| 2-((3-(2-amino-2-carboxyethyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6h)-yl)methyl)benzoic acid |
| 2-[[3-(2-amino-2-carboxyethyl)-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid |
| ubp296 |
| CS-0028946 |
| HY-107605 |
Research Excerpts
Overview
UBP296 was found to be a potent and selective antagonist of native GLUK5-containing kainate receptors in the spinal cord, with activity residing in the S enantiomer (UBP302)
| Excerpt | Reference | Relevance |
|---|---|---|
| "UBP296 was found to be a potent and selective antagonist of native GLUK5-containing kainate receptors in the spinal cord, with activity residing in the S enantiomer (UBP302)." | ( Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Alt, AJ; Bleakman, D; Bortolotto, ZA; Buelens, FP; Clarke, VR; Collingridge, GL; Dolman, NP; Jane, DE; Kelland, EE; More, JC; Nistico, R; Ogden, AM; Pilato, F; Troop, HM, 2004) | 1.37 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| alpha-amino acid | An amino acid in which the amino group is located on the carbon atom at the position alpha to the carboxy group. |
| [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 (8)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 97.6000 | 0.0001 | 1.6179 | 10.0000 | AID257196 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 97.6000 | 0.0001 | 1.7000 | 10.0000 | AID257196 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 97.6000 | 0.0001 | 1.7000 | 10.0000 | AID257196 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 97.6000 | 0.0001 | 1.7000 | 10.0000 | AID257196 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | Ki | 1,000.0000 | 0.0037 | 0.8025 | 4.1000 | AID257202 |
| Glutamate receptor ionotropic, kainate 3 | Homo sapiens (human) | IC50 (µMol) | 880.0000 | 0.0770 | 2.0385 | 4.0000 | AID257203 |
| Glutamate receptor ionotropic, kainate 3 | Homo sapiens (human) | Ki | 374.0000 | 0.0100 | 0.3995 | 0.7890 | AID257203 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | Kd | 1.0900 | 0.0180 | 1.2720 | 3.9400 | AID257198 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, kainate 1 | Homo sapiens (human) | Kb | 0.6000 | 0.0080 | 0.4030 | 1.0000 | AID257204 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (16)
Molecular Functions (7)
Ceullar Components (11)
Bioassays (15)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID257200 | Displacement of [3H](S)-5-fluorowillardiine from AMPA receptor in rat brain membrane | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257210 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUA2 receptor expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257208 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUK6/GLUK2 receptor clone expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257203 | Displacement of [3H]kainate from human GLUK7 receptor expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257202 | Displacement of [3H]kainate from rat GLUK6 receptor expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257196 | Antagonist activity on AMPA receptor expressed on rat motoneurons by its ability to reduce the fast component dorsal root evoked ventral root potential (fDR-VRP) | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257201 | Displacement of [3H]SYM2081 from kainate receptor in rat brain membrane | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257209 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUA1 receptor expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257204 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUK5 receptor expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257198 | Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257205 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUK5/GLUK2 receptor clone expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257206 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUK5/GLUK6 receptor clone expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257207 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUK6 receptor expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257211 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUA3 receptor expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| AID257212 | Inhibitory effect on glutamate-induced calcium influx at homomeric human GLUA4 receptor expressed in HEK293 cells up to 300 uM | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (60.00) | 29.6817 |
| 2010's | 2 (40.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||