LY 465608: a nonthiazolidinedione agonist of both PPAR-alpha and PPAR-gamma of Ligand Pharm. and Eli Lilly [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9890319 |
| CHEMBL ID | 25259 |
| SCHEMBL ID | 6695462 |
| MeSH ID | M0423292 |
| Synonym |
|---|
| gtpl2659 |
| 2-methyl-2-[4-[2-[5-methyl-2-(4-phenylphenyl)-1,3-oxazol-4-yl]ethoxy]phenoxy]propanoic acid |
| ly465608 |
| ly-465608 |
| ly 465608 |
| CHEMBL25259 , |
| 2-{4-[2-(2-biphenyl-4-yl-5-methyl-oxazol-4-yl)-ethoxy]-phenoxy}-2-methyl-propionic acid |
| bdbm50100442 |
| AKOS005067136 |
| JDJHTJNBMZSSLK-UHFFFAOYSA-N |
| 2-methyl-2-{4-[2-(5-methyl-2-biphenyl-4-yl-oxazol-4-yl)ethoxy]phenoxy}propionic acid |
| SCHEMBL6695462 |
| Q27083155 |
| 328918-26-9 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Repeat-dose nonclinical safety studies of LY465608 revealed abnormities in mitochondrial morphology and evidence of single-cell necrosis following 30 days of dosing exclusively in dogs, but not in rats." | ( Underlying mechanisms of pharmacology and toxicity of a novel PPAR agonist revealed using rodent and canine hepatocytes. Baker, TK; Calley, JN; Gao, H; Guo, Y; Halstead, BW; Huffman, M; Irizarry, AR; Jolly, RA; Li, S; Qian, HR; Ryan, TP; Searfoss, GH; Stevens, JL; Stutz, JP; West, A, 2007) | 0.34 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | IC50 (µMol) | 0.5480 | 0.0050 | 1.2051 | 10.0000 | AID223558 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Ki | 0.5500 | 0.0000 | 0.3790 | 5.6000 | AID238857 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | IC50 (µMol) | 0.1740 | 0.0005 | 0.8269 | 6.3100 | AID223553 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | Ki | 0.1700 | 0.0001 | 1.0189 | 4.5000 | AID238856 |
| ATP-binding cassette sub-family C member 8 | Homo sapiens (human) | IC50 (µMol) | 0.5480 | 0.0043 | 1.0703 | 8.2000 | AID223558 |
| ATP-sensitive inward rectifier potassium channel 11 | Homo sapiens (human) | IC50 (µMol) | 0.5480 | 0.0043 | 1.3686 | 8.2000 | AID223558 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | EC50 (µMol) | 0.1500 | 0.0020 | 0.4753 | 3.2000 | AID240312 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | EC50 (µMol) | 0.8807 | 0.0000 | 0.9922 | 10.0000 | AID156797; AID223555; AID240313 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | EC50 (µMol) | 0.1498 | 0.0006 | 1.6074 | 10.0000 | AID155986; AID223550; AID240312 |
| ATP-binding cassette sub-family C member 8 | Homo sapiens (human) | EC50 (µMol) | 0.1495 | 0.0219 | 1.1257 | 8.8000 | AID223550 |
| ATP-sensitive inward rectifier potassium channel 11 | Homo sapiens (human) | EC50 (µMol) | 0.1495 | 0.0219 | 0.9708 | 8.8000 | AID223550 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID493017 | Wombat Data for BeliefDocking | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID240312 | Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. |
| AID155986 | Agonistic activity for Peroxisome proliferator activated receptor alpha | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. |
| AID223553 | Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID223558 | Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID240313 | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. |
| AID238857 | Binding affinity for human peroxisome proliferator activated receptor gamma | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. |
| AID238856 | Binding affinity for human peroxisome proliferator activated receptor alpha | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. |
| AID223557 | Transcriptional activation in CV- cells expressing hPPARgamma | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID223555 | Binding affinity at human PPAR gamma | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID223550 | Binding affinity at human PPAR alpha | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID223552 | Transcriptional activation in CV-1 cells expressing hPPARalpha | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID156797 | Agonistic activity for human Peroxisome proliferator activated receptor gamma | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. |
| AID1346733 | Human Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-activated receptors) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| AID1346733 | Human Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-activated receptors) | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists. |
| AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (100.00) | 29.6817 |
| 2010's | 0 (0.00) | 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] | ||
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 (12.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (14.29%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (85.71%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||