LY2183240: structure in first source [MeSH]
N,N-dimethyl-5-[(4-phenylphenyl)methyl]-1-tetrazolecarboxamide : no description available [CHeBI]
ID Source | ID |
---|---|
PubMed CID | 11507802 |
CHEMBL ID | 509860 |
SCHEMBL ID | 2184828 |
CHEBI ID | 92670 |
MeSH ID | M0513545 |
Synonym |
---|
n,n-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide |
HY-10865 |
HMS3269E15 |
NCGC00159571-01 |
chembl509860 , |
bdbm26736 |
ly2183240 |
n,n-dimethyl-5-[(4-phenylphenyl)methyl]-1h-1,2,3,4-tetrazole-1-carboxamide |
ly-2183240 |
874902-19-9 |
BCP9000870 |
ly2183240/ly-2183240 |
BCP0726000083 |
5-biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide |
LP01268 |
CS-0913 |
BRD-K37865504-001-01-7 |
5-([1,1'-biphenyl]-4-ylmethyl)-n,n-dimethyl-1h-tetrazole-1-carboxamide |
SCHEMBL2184828 |
5-[(1,1'-biphenyl]-4-yl)methyl]-n,n-dimethyl-1h-tetrazole-1-carboxamide |
ly 2183240 |
AKOS024457108 |
CHEBI:92670 |
2WBU91OKM7 , |
5-(biphenyl-4-ylmethyl)-n,n-dimethyl-1h-tetrazole-1-carboxamide |
1h-tetrazole-1-carboxamide, 5-((1,1'-biphenyl)-4-ylmethyl)-n,n-dimethyl- |
ly-2183240; ly 2183240 |
BCP22610 |
unii-2wbu91okm7 |
HMS3677O06 |
HMS3413O06 |
n,n-dimethyl-5-[(4-phenylphenyl)methyl]-1-tetrazolecarboxamide |
Q6460409 |
SDCCGSBI-0633820.P001 |
F84861 |
EX-A4760 |
S8052 |
DTXSID001024706 |
5-((1,1'-biphenyl)-4-ylmethyl)-n,n-dimethyl-1h-tetrazole-1-carboxamide |
AS-82203 |
AC-36729 |
5-[[(1,1'-biphenyl)-4-yl]methyl]-n,n-dimethyl-1h-tetrazole-1-carboxamide |
Class | Description |
---|---|
biphenyls | Benzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond. |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 1.0000 | AID1030 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Fatty-acid amide hydrolase 1 | Homo sapiens (human) | IC50 | 0.0248 | AID439742; AID441698; AID612783; AID726796 |
Fatty-acid amide hydrolase 1 | Mus musculus (house mouse) | IC50 | 0.0130 | AID1798722 |
Monoglyceride lipase | Mus musculus (house mouse) | IC50 | 0.0045 | AID1798723 |
Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 | 0.0099 | AID346665; AID612777; AID743631 |
Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | Ki | 0.0120 | AID412539 |
Transient receptor potential cation channel subfamily A member 1 | Rattus norvegicus (Norway rat) | IC50 | 49.4000 | AID743747 |
Neutral cholesterol ester hydrolase 1 | Mus musculus (house mouse) | IC50 | 0.0045 | AID1798723 |
Transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | IC50 | 100.0000 | AID743741 |
Monoacylglycerol lipase ABHD6 | Mus musculus (house mouse) | IC50 | 0.0045 | AID1798723 |
Monoglyceride lipase | Homo sapiens (human) | IC50 | 0.1331 | AID439741; AID441697; AID743632 |
Diacylglycerol lipase-alpha | Homo sapiens (human) | IC50 | 10.0000 | AID382401 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Transient receptor potential cation channel subfamily A member 1 | Rattus norvegicus (Norway rat) | EC50 | 26.9000 | AID743739 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID441792 | Selectivity ratio for human MGL activity to human recombinant FAAH | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804 | Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors. |
AID743740 | Agonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis relative to allyl isothiocyanate | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID612783 | Inhibition of FAAH | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 ISSN: 1464-3405 | The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH). |
AID382405 | Inhibition of [14C]anandamide uptake in rat RBL-2H3 cells preincubated 10 mins before addition of [14C]anandamide | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID743632 | Inhibition of human recombinant MAGL-mediated 1,3-dihydroxypropan-1-yl 4-pyren-1-ylbutanoate conversion to 4-pyren-1-ylbutanoic acid preincubated for 15 mins measured after 45 mins by HPLC analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | (4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). |
AID612777 | Inhibition of rat FAAH | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 ISSN: 1464-3405 | The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH). |
AID382407 | Inhibition of [14C]anandamide uptake in rat RBL-2H3 cells at 1 uM preincubated 10 mins before addition of [14C]anandamide | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID346665 | Inhibition of rat FAAH | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 ISSN: 1520-4804 | Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors. |
AID382404 | Inhibition of FAAH mediated [14C]anandamide hydrolysis in rat brain at 1 uM after 30 mins | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID743628 | Selectivity ratio of IC50 for human recombinant MAGL to IC50 for FAAH in Sprague-Dawley rat brain microsomes | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | (4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). |
AID441698 | Inhibition of human recombinant FAAH-maltose binding protein | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804 | Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors. |
AID439742 | Inhibition of human FAAH | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 ISSN: 1520-4804 | Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. |
AID743626 | Inhibition of cytosolic phospholipase A2alpha in porcine platelets assessed as 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine conversion to arachidonic acid at 10 uM by HPLC analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | (4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). |
AID743631 | Inhibition of FAAH in Sprague-Dawley rat brain microsomes assessed as N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide conversion to 4-pyren-1-ylbutanoic acid preincubated for 10 mins measured after 45 mins by HPLC analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | (4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). |
AID743747 | Antagonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular Ca2+ elevation incubated for 5 mins prior to allyl isothiocyanate-stimulation by spectrofluorimetric analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID441697 | Inhibition of human MGL activity using [3H]2-oleoylglycerol substrate by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804 | Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors. |
AID382403 | Inhibition of FAAH mediated [14C]anandamide hydrolysis in rat brain at 0.1 uM after 30 mins | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID743742 | Agonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID726796 | Inhibition of FAAH (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 ISSN: 1464-3391 | Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors. |
AID382400 | Inhibition of MAGL mediated [14C]2-arachidonoyl glycerol hydrolysis in african green monkey COS cells | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID743739 | Agonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID382406 | Inhibition of [14C]anandamide uptake in rat RBL-2H3 cells at 0.1 uM preincubated 10 mins before addition of [14C]anandamide | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID439743 | Selectivity ratio of IC50 for human FAAH to IC50 for human MGL | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 ISSN: 1520-4804 | Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. |
AID1363883 | Inhibition of mouse brain membrane FAAH preincubated for 10 mins followed by 14C-oleamide substrate addition measured up to 60 mins by TLC analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 ISSN: 1520-4804 | Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors. |
AID382402 | Inhibition of FAAH mediated [14C]anandamide hydrolysis in rat brain after 30 mins | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID382401 | Inhibition of human recombinant DAGLalpha mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in COS cells after 20 mins | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 ISSN: 0223-5234 | Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. |
AID743743 | Agonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis relative to ionomycin | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID439741 | Inhibition of human MGL | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 ISSN: 1520-4804 | Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. |
AID743741 | Antagonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ elevation incubated for 5 mins prior to capsaicin-stimulation by spectrofluorimetric analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63ISSN: 1768-3254 | Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring. |
AID412539 | Inhibition of rat cortex FAAH by [3H]anandamide carbon filtration assay | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 ISSN: 1520-4804 | Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 ISSN: 2211-1247 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347154 | Primary screen GU AMC 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1798723 | Serine Hydrolase Activity Assay from Article 10.1021/ja062999h: \\The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.\\ | 2006 | Journal of the American Chemical Society, Aug-02, Volume: 128, Issue:30 ISSN: 0002-7863 | The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. |
AID1798722 | FAAH Competitive ABPP Using FP-Rhodamine from Article 10.1021/ja062999h: \\The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.\\ | 2006 | Journal of the American Chemical Society, Aug-02, Volume: 128, Issue:30 ISSN: 0002-7863 | The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 6 (33.33) | 29.6817 |
2010's | 9 (50.00) | 24.3611 |
2020's | 3 (16.67) | 2.80 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 3 (16.67%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 15 (83.33%) | 84.16% |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Absence Seizure | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Ache | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Alcohol Drinking | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Anxiety | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Chemical Dependence | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Disease Models, Animal | 0 | 2010 | 2020 | 8.0 | high | 0 | 0 | 0 | 1 | 2 | 0 | |
Pain | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Seizures | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Substance-Related Disorders | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Article | Year |
---|---|
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors. Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1 | 2013 |