Page last updated: 2024-11-12
ro 4956371
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine: a metabotropic glutamate receptor 5 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11646823 |
| CHEMBL ID | 3410223 |
| SCHEMBL ID | 608379 |
| MeSH ID | M0569931 |
Synonyms (43)
| Synonym |
|---|
| 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine |
| HY-15445 |
| CS-0974 |
| ctep |
| S2861 |
| [3h]ctep |
| gtpl6409 |
| compound 3 [pmid: 25565255] |
| gtpl6408 |
| SCHEMBL608379 |
| AM808005 |
| 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1h-imidazol-4-yl)ethynyl)pyridine |
| 871362-31-1 |
| c19h13clf3n3o |
| ctep (ro4956371) |
| ro 4956371 |
| DTXSID50469986 |
| bdbm50071375 |
| J-690373 |
| CHEMBL3410223 , |
| EX-A095 |
| AKOS027301517 |
| HMS3651N19 |
| mglur5 inhibitor |
| ro4956371 |
| NCGC00386156-06 |
| gohctcogykajlz-uhfffaoysa-n |
| SW219465-1 |
| FT-0749890 |
| BCP06140 |
| Q5014559 |
| mfcd22665726 |
| AS-17058 |
| ro 4956371;mglur5 inhibitor |
| HMS3884J20 |
| CCG-268547 |
| I10317 |
| unii-e3bwg5775s |
| pyridine, 2-chloro-4-(2-(2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1h-imidazol-4-yl)ethynyl)- |
| 2-chloranyl-4-(2-(2,5-dimethyl-1-(4-(trifluoromethyloxy)phenyl)imidazol-4-yl)ethynyl)pyridine |
| e3bwg5775s , |
| A922951 |
| AC-35775 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Here, we present the novel potent, selective, and orally bioavailable mGlu5 negative allosteric modulator with inverse agonist properties 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine (CTEP)." | ( CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. Büttelmann, B; Diener, C; Fischer, C; Flament, C; Gatti, S; Hartung, T; Hoffmann, G; Honer, M; Jaeschke, G; Kolczewski, S; Lindemann, L; Michalon, A; Parrott, N; Porter, R; Prinssen, EP; Spooren, W; Vieira, E; Wettstein, JG, 2011) | 0.37 |
| " Chronic administration of the selective and orally bioavailable mGluR5 inverse agonist, CTEP, was able to recover behavioral alterations induced by chronic stress, whereas overexpression of Homer1a in the hippocampus led to an increased vulnerability to chronic stress, reflected in an increased physiological response to stress as well as enhanced depression-like behavior." | ( Homer1/mGluR5 activity moderates vulnerability to chronic social stress. Gassen, NC; Harbich, D; Hartmann, J; Häusl, AS; Jaschke, G; Kohl, C; Labermaier, C; Lindemann, L; Matosin, N; Müller, MB; Rein, T; Santarelli, S; Schieven, M; Schmid, B; Schmidt, MV; Turck, CW; Wagner, KV; Wang, XD; Webhofer, C; Wettstein, JG; Zhao, G, 2015) | 0.42 |
| " Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in APPswe/PS1ΔE9 mice and reduces Aβ plaque deposition and soluble Aβ oligomer concentrations in both APPswe/PS1ΔE9 and 3xTg-AD male mice." | ( Chronic Pharmacological mGluR5 Inhibition Prevents Cognitive Impairment and Reduces Pathogenesis in an Alzheimer Disease Mouse Model. Anisman, H; Ferguson, SS; Hamilton, A; McQuaid, RJ; Vander Tuin, C; Vasefi, M, 2016) | 0.43 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (25)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.6840 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 8.4866 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
Biological Processes (110)
Molecular Functions (51)
Ceullar Components (57)
Bioassays (32)
Research
Studies (21)
| 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 | 18 (85.71) | 24.3611 |
| 2020's | 3 (14.29) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.42
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 weak demand-to-supply ratio for research on this compound.
| This Compound (11.42) All Compounds (24.57) |
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 | 21 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||