Page last updated: 2024-11-13
urb937
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
URB937: a peripherally restricted inhibitor of fatty acid amide hydrolase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 53394762 |
| CHEMBL ID | 2402927 |
| SCHEMBL ID | 528582 |
| MeSH ID | M0550918 |
Synonyms (22)
| Synonym |
|---|
| bdbm50437227 |
| chembl2402927 , |
| SCHEMBL528582 |
| cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester |
| urb937 |
| 1357160-72-5 |
| 3'-carbamoyl-6-hydroxybiphenyl-3-yl cyclohexylcarbamate |
| urb-937 |
| AKOS027422596 |
| CS-0065602 |
| HY-116477 |
| NCGC00351474-02 |
| urb 937 |
| 3'-(aminocarbonyl)-6-hydroxy[1,1'-biphenyl]-3-yl n-cyclohexylcarbamate |
| EX-A4088 |
| DTXSID801018151 |
| gtpl11817 |
| A936336 |
| 3'-carbamoyl-6-hydroxy-[1,1'-biphenyl]-3-yl cyclohexylcarbamate |
| MS-25529 |
| [3-(3-carbamoylphenyl)-4-hydroxyphenyl] n-cyclohexylcarbamate |
| AC-36524 |
Research Excerpts
Overview
URB937 is a peripherally restricted inhibitor of the anandamide-deactivating enzyme fatty-acid amide hydrolase (FAAH)
| Excerpt | Reference | Relevance |
|---|---|---|
| "URB937 is a peripherally restricted inhibitor of the anandamide-deactivating enzyme fatty-acid amide hydrolase (FAAH). " | ( Pharmacological characterization of the peripheral FAAH inhibitor URB937 in female rodents: interaction with the Abcg2 transporter in the blood-placenta barrier. Bertorelli, R; Guijarro, A; Moreno-Sanz, G; Oluyemi, O; Piomelli, D; Reggiani, A; Sasso, O, 2012) | 2.06 |
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with URB937 decreased leukocyte migration and inflammatory cytokines in bronchoalveolar lavage fluid and plasma at day 30." | ( The Fatty Acid Amide Hydrolase Inhibitor URB937 Ameliorates Radiation-Induced Lung Injury in a Mouse Model. Chen, G; Deng, L; Lan, J; Li, R; Lu, Y; Tang, F; Tong, R; Xu, H; Xue, J; Zhou, L, 2017) | 1.06 |
Pharmacokinetics
The favourable pharmacokinetic and pharmacodynamic properties of URB937, along with its tolerability, encourage further development studies on this compound.
| Excerpt | Reference | Relevance |
|---|---|---|
| " We examined, in rats, (1) the pharmacokinetic profile of oral URB937; (2) the compound's ability to elevate levels of the representative FAAH substrate, oleoylethanolamide (OEA); and (3) the compound's tolerability after oral administration." | ( Pharmacokinetics, pharmacodynamics and safety studies on URB937, a peripherally restricted fatty acid amide hydrolase inhibitor, in rats. Ahmed, F; Choobchian, P; Duranti, A; Merrill, CB; Mor, M; Piomelli, D; Rivara, S; Tarzia, G; Tontini, A; Vozella, V; Zibardi, C, 2019) | 1 |
| " The favourable pharmacokinetic and pharmacodynamic properties of URB937, along with its tolerability, encourage further development studies on this compound." | ( Pharmacokinetics, pharmacodynamics and safety studies on URB937, a peripherally restricted fatty acid amide hydrolase inhibitor, in rats. Ahmed, F; Choobchian, P; Duranti, A; Merrill, CB; Mor, M; Piomelli, D; Rivara, S; Tarzia, G; Tontini, A; Vozella, V; Zibardi, C, 2019) | 1 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0020 | 0.0003 | 0.7123 | 7.0700 | AID759738 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0020 | 0.0005 | 1.3313 | 8.0000 | AID759738 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Bioassays (16)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1363878 | Inhibition of FAAH in Wistar rat brain membranes using [3H]-anandamide as substrate preincubated for 10 mins followed by substrate addition measured after 4 mins by liquid scintillation counting method | 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. |
| AID759729 | In vivo inhibition of FAAH in sc dosed Swiss Webster mouse brain using [3H]-ethanolamine as substrate after 1 hr by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759724 | Selectivity ratio of ED50 for inhibition of FAAH in ip dosed Swiss Webster mouse brain to ED50 for inhibition of FAAH in ip dosed Swiss Webster mouse peripheral tissue | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759733 | In vivo inhibition of FAAH in ip dosed Swiss Webster mouse brain using [3H]-ethanolamine as substrate after 1 hr by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759738 | Inhibition of Wistar rat brain FAAH using [3H]-ethanolamine as substrate preincubated for 20 mins followed by substrate addition by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759732 | In vivo inhibition of FAAH in Swiss Webster mouse brain using [3H]-ethanolamine as substrate at 25 mg/kg, sc after 1 hr by liquid scintillation counting analysis in presence of Abcg2 inhibitor Ko-143 | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759727 | In vivo inhibition of FAAH in ip dosed Swiss Webster mouse liver | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759735 | In vivo inhibition of FAAH in Swiss Webster mouse brain using [3H]-ethanolamine as substrate at 1 mg/kg, ip after 1 hr by liquid scintillation counting analysis relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759737 | In vivo inhibition of FAAH in Swiss Webster mouse liver using [3H]-ethanolamine as substrate at 1 mg/kg, ip after 1 hr by liquid scintillation counting analysis relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759726 | Selectivity ratio of ED50 for inhibition of FAAH in ip dosed Swiss Webster mouse brain to ED50 for inhibition of FAAH in ip dosed Swiss Webster mouse liver | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| AID759725 | In vivo inhibition of FAAH in ip dosed Swiss Webster mouse peripheral tissue | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (23)
| 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 | 19 (82.61) | 24.3611 |
| 2020's | 4 (17.39) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 20.73
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (20.73) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (4.17%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 23 (95.83%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||