CAY10499
monoglyceride lipase inhibitor (IC50 144 nM) but inhibits also ATGL (not an alpha/beta hydrolase) HSL, DAGLA ABHD6 and CES1 (Iglesias et al 2016)
General
Chemical_Nomenclature : benzyl N-[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3-yl)-2-methylphenyl]carbamate
Canonical SMILES : CC1=C(C=CC(=C1)N2C(=O)OC(=N2)OC)NC(=O)OCC3=CC=CC=C3
InChI : InChI=1S\/C18H17N3O5\/c1-12-10-14(21-18(23)26-17(20-21)24-2)8-9-15(12)19-16(22)25-11-13-6-4-3-5-7-13\/h3-10H,11H2,1-2H3,(H,19,22)
InChIKey : QTENHWTVRQKWRI-UHFFFAOYSA-N
Other name(s) : CHEMBL570812 || CAY-10499 || SCHEMBL7042914 || ZINC592819 || BDBM50414921
MW : 355.34
Formula : C18H17N3O5
CAS_number :
PubChem : 9924775
UniChem : QTENHWTVRQKWRI-UHFFFAOYSA-N
Target
Families : CAY10499 ligand of proteins in family
Monoglyceridelipase_lysophospholip
Carb_B_Chordata
ABHD6-Lip
Lipase_3
Hormone-sensitive_lipase_like
Protein :
human-MGLL
References (15)
| Title : Novel Pharmacological Probes Reveal ABHD5 as a Locus of Lipolysis Control in White and Brown Adipocytes - Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| Author(s) : Rondini EA , Mladenovic-Lucas L , Roush WR , Halvorsen GT , Green AE , Granneman JG |
| Ref : Journal of Pharmacology & Experimental Therapeutics , 363 :367 , 2017 |
| Abstract : |
| PubMedSearch : Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| PubMedID: 28928121 |
| Gene_locus related to this paper: human-ABHD5 , mouse-abhd5 |
| Title : Novel Pharmacological Probes Reveal ABHD5 as a Locus of Lipolysis Control in White and Brown Adipocytes - Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| Author(s) : Rondini EA , Mladenovic-Lucas L , Roush WR , Halvorsen GT , Green AE , Granneman JG |
| Ref : Journal of Pharmacology & Experimental Therapeutics , 363 :367 , 2017 |
| Abstract : |
| PubMedSearch : Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| PubMedID: 28928121 |
| Gene_locus related to this paper: human-ABHD5 , mouse-abhd5 |
| Title : Novel Pharmacological Probes Reveal ABHD5 as a Locus of Lipolysis Control in White and Brown Adipocytes - Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| Author(s) : Rondini EA , Mladenovic-Lucas L , Roush WR , Halvorsen GT , Green AE , Granneman JG |
| Ref : Journal of Pharmacology & Experimental Therapeutics , 363 :367 , 2017 |
| Abstract : |
| PubMedSearch : Rondini_2017_J.Pharmacol.Exp.Ther_363_367 |
| PubMedID: 28928121 |
| Gene_locus related to this paper: human-ABHD5 , mouse-abhd5 |
| Title : Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors - Iglesias_2016_J.Lipid.Res_57_131 |
| Author(s) : Iglesias J , Lamontagne J , Erb H , Gezzar S , Zhao S , Joly E , Truong VL , Skorey K , Crane S , Madiraju SR , Prentki M |
| Ref : J Lipid Res , 57 :131 , 2016 |
| Abstract : |
| PubMedSearch : Iglesias_2016_J.Lipid.Res_57_131 |
| PubMedID: 26423520 |
| Title : Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors - Iglesias_2016_J.Lipid.Res_57_131 |
| Author(s) : Iglesias J , Lamontagne J , Erb H , Gezzar S , Zhao S , Joly E , Truong VL , Skorey K , Crane S , Madiraju SR , Prentki M |
| Ref : J Lipid Res , 57 :131 , 2016 |
| Abstract : |
| PubMedSearch : Iglesias_2016_J.Lipid.Res_57_131 |
| PubMedID: 26423520 |
| Title : Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors - Iglesias_2016_J.Lipid.Res_57_131 |
| Author(s) : Iglesias J , Lamontagne J , Erb H , Gezzar S , Zhao S , Joly E , Truong VL , Skorey K , Crane S , Madiraju SR , Prentki M |
| Ref : J Lipid Res , 57 :131 , 2016 |
| Abstract : |
| PubMedSearch : Iglesias_2016_J.Lipid.Res_57_131 |
| PubMedID: 26423520 |
| Title : Dual inhibition of MAGL and type II topoisomerase by N-phenylmaleimides as a potential strategy to reduce neuroblastoma cell growth - Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| Author(s) : Matuszak N , Hamtiaux L , Baldeyroux B , Muccioli GG , Poupaert JH , Lansiaux A , Lambert DM |
| Ref : Eur J Pharm Sci , 45 :263 , 2012 |
| Abstract : |
| PubMedSearch : Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| PubMedID: 22127371 |
| Title : Dual inhibition of MAGL and type II topoisomerase by N-phenylmaleimides as a potential strategy to reduce neuroblastoma cell growth - Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| Author(s) : Matuszak N , Hamtiaux L , Baldeyroux B , Muccioli GG , Poupaert JH , Lansiaux A , Lambert DM |
| Ref : Eur J Pharm Sci , 45 :263 , 2012 |
| Abstract : |
| PubMedSearch : Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| PubMedID: 22127371 |
| Title : Dual inhibition of MAGL and type II topoisomerase by N-phenylmaleimides as a potential strategy to reduce neuroblastoma cell growth - Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| Author(s) : Matuszak N , Hamtiaux L , Baldeyroux B , Muccioli GG , Poupaert JH , Lansiaux A , Lambert DM |
| Ref : Eur J Pharm Sci , 45 :263 , 2012 |
| Abstract : |
| PubMedSearch : Matuszak_2012_Eur.J.Pharm.Sci_45_263 |
| PubMedID: 22127371 |
| Title : Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescence-based technique - Savinainen_2010_Anal.Biochem_399_132 |
| Author(s) : Savinainen JR , Yoshino M , Minkkila A , Nevalainen T , Laitinen JT |
| Ref : Analytical Biochemistry , 399 :132 , 2010 |
| Abstract : |
| PubMedSearch : Savinainen_2010_Anal.Biochem_399_132 |
| PubMedID: 20005861 |
| Gene_locus related to this paper: human-MGLL |
| Title : Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescence-based technique - Savinainen_2010_Anal.Biochem_399_132 |
| Author(s) : Savinainen JR , Yoshino M , Minkkila A , Nevalainen T , Laitinen JT |
| Ref : Analytical Biochemistry , 399 :132 , 2010 |
| Abstract : |
| PubMedSearch : Savinainen_2010_Anal.Biochem_399_132 |
| PubMedID: 20005861 |
| Gene_locus related to this paper: human-MGLL |
| Title : Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescence-based technique - Savinainen_2010_Anal.Biochem_399_132 |
| Author(s) : Savinainen JR , Yoshino M , Minkkila A , Nevalainen T , Laitinen JT |
| Ref : Analytical Biochemistry , 399 :132 , 2010 |
| Abstract : |
| PubMedSearch : Savinainen_2010_Anal.Biochem_399_132 |
| PubMedID: 20005861 |
| Gene_locus related to this paper: human-MGLL |
| Title : CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay - Muccioli_2008_Chembiochem_9_2704 |
| Author(s) : Muccioli GG , Labar G , Lambert DM |
| Ref : Chembiochem , 9 :2704 , 2008 |
| Abstract : |
| PubMedSearch : Muccioli_2008_Chembiochem_9_2704 |
| PubMedID: 18855964 |
| Gene_locus related to this paper: human-MGLL |
| Title : CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay - Muccioli_2008_Chembiochem_9_2704 |
| Author(s) : Muccioli GG , Labar G , Lambert DM |
| Ref : Chembiochem , 9 :2704 , 2008 |
| Abstract : |
| PubMedSearch : Muccioli_2008_Chembiochem_9_2704 |
| PubMedID: 18855964 |
| Gene_locus related to this paper: human-MGLL |
| Title : CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay - Muccioli_2008_Chembiochem_9_2704 |
| Author(s) : Muccioli GG , Labar G , Lambert DM |
| Ref : Chembiochem , 9 :2704 , 2008 |
| Abstract : |
| PubMedSearch : Muccioli_2008_Chembiochem_9_2704 |
| PubMedID: 18855964 |
| Gene_locus related to this paper: human-MGLL |