| ID Source | ID |
|---|---|
| PubMed CID | 9972176 |
| CHEMBL ID | 257307 |
| CHEBI ID | 188240 |
| SCHEMBL ID | 3964457 |
| Synonym |
|---|
| CHEMBL257307 , |
| cay10435 |
| 1-([1,3]oxazolo[4,5-b]pyridin-2-yl)dodecan-1-one |
| CHEBI:188240 |
| bdbm50350547 |
| SCHEMBL3964457 |
| 288862-73-7 |
| 1-oxazolo[4,5-b]pyridin-2-yl-1-dodecanone |
| HMS3649B18 |
| 1-[1,3]oxazolo[4,5-b]pyridin-2-yldodecan-1-one |
| 1-(oxazolo[4,5-b]pyridin-2-yl)dodecan-1-one |
| SR-01000946699-1 |
| sr-01000946699 |
| 1-oxaxolo[4,5-b]pyridin-2-yl-1-dodecanone |
| Excerpt | Reference | Relevance |
|---|---|---|
| " For example, 6e is an orally active inhibitor of human neutrophil elastase that entered human clinical studies, 52h is an orally bioavailable inhibitor of human chymase, and 82m is a FAAH inhibitor with in vivo endocannabinoid-enhancing activity." | ( Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. Costanzo, MJ; Maryanoff, BE, 2008) | 0.35 |
| Class | Description |
|---|---|
| oxazolopyridine | |
| [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 | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fatty-acid amide hydrolase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0168 | 0.0002 | 0.5982 | 7.0000 | AID1053388 |
| Fatty-acid amide hydrolase 1 | Homo sapiens (human) | Ki | 0.0006 | 0.0006 | 1.2747 | 6.0000 | AID612783 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 0.0006 | 0.1619 | 2.0000 | AID1363877; AID321257 |
| Diacylglycerol lipase-alpha | Homo sapiens (human) | IC50 (µMol) | 0.0309 | 0.0010 | 1.0538 | 5.0119 | AID1270928 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein binding | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| phospholipid binding | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| fatty acid amide hydrolase activity | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| identical protein binding | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| acylglycerol lipase activity | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| amidase activity | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| protein binding | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| metal ion binding | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| acylglycerol lipase activity | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| lipoprotein lipase activity | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| endoplasmic reticulum membrane | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| cytoskeleton | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| organelle membrane | Fatty-acid amide hydrolase 1 | Homo sapiens (human) |
| plasma membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| early endosome membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| dendrite membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| dendritic spine membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| varicosity | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| postsynaptic density membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| dendrite membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| cytoplasm | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| postsynaptic membrane | Diacylglycerol lipase-alpha | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID321257 | Inhibition of rat FAAH | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID1053388 | Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate preincubated for 10 mins before substrate addition measured after 10 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors. |
| AID612783 | Inhibition of FAAH | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH). |
| AID321259 | Selectivity for rat FAAH over triacylglycerol hydrolase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID1053380 | Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate at 30 uM preincubated for 10 to 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors. |
| AID1053379 | Reversible inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using arachidonic acid as substrate assessed as recovery of enzyme activity at 20 x IC50 preincubated for 60 mins followed by 500 fold dilution measured after | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors. |
| AID1270928 | Inhibition of full-length human DAGLalpha expressed in HEK293T cell membranes using para-nitrophenylbutyrate by colorimetric assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24 | Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors. |
| AID1363877 | Inhibition of rat FAAH assessed as reduction in [14C]oleamide conversion to oleic acid by Lineweaver-Burk plot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors. |
| [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 | 1 (20.00) | 29.6817 |
| 2010's | 4 (80.00) | 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] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (60.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 2 (40.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||