LIPG-inhib-Compound32

mPlasma IC50 120 nM, human-LIPG (endothelial) EL IC50 4.6 (nM), human-LIPC (hepatic) HL IC50 230 (nM)

General

Type : Pyridine, Benzothiazol, Sulfur Compound, Sulfonyl, Cyclopropyl

Chemical_Nomenclature : N-[(cyclopropylcarbamoyl)methyl]-2-[6-(6-fluoropyridin-3-yl)-1,3-benzothiazol-2-yl]-2-(2-methoxyethanesulfonyl)acetamide

Canonical SMILES : C1=C(N=CC(=C1)C2=CC3=C(C=C2)N=C(S3)C(C(=O)CNC(NC4CC4)=O)[S](CCOC)(=O)=O)F

InChI : InChI=1S\/C22H23FN4O5S2\/c1-32-8-9-34(30,31)20(17(28)12-25-22(29)26-15-4-5-15)21-27-16-6-2-13(10-18(16)33-21)14-3-7-19(23)24-11-14\/h2-3,6-7,10-11,15,20H,4-5,8-9,12H2,1H3,(H2,25,26,29)

InChIKey : GKMCWXRBVOBYGF-UHFFFAOYSA-N

Other name(s) :


MW : 506.56

Formula : C22H23FN4O5S2

CAS_number :

PubChem :

UniChem : GKMCWXRBVOBYGF-UHFFFAOYSA-N

Target

Families : LIPG-inhib-Compound32 ligand of proteins in family
Lipoprotein_Lipase

Protein :
human-LIPG

References (2)

Title : Benzothiazole-based compounds as potent endothelial lipase inhibitors - Meng_2019_Bioorg.Med.Chem.Lett__126673
Author(s) : Meng W , Adam LP , Behnia K , Zhao L , Yang R , Kopcho LM , Locke GA , Taylor DS , Yin X , Wexler RR , Finlay H
Ref : Bioorganic & Medicinal Chemistry Lett , :126673 , 2019
Abstract :
PubMedSearch : Meng_2019_Bioorg.Med.Chem.Lett__126673
PubMedID: 31519373
Gene_locus related to this paper: human-LIPG

Title : Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase - Kim_2019_Bioorg.Med.Chem.Lett_29_1918
Author(s) : Kim SH , Johnson JA , Jiang J , Parkhurst B , Phillips M , Pi Z , Qiao JX , Tora G , Ye Chen A , Liu E , Yin X , Yang R , Zhao L , Taylor DS , Basso M , Behnia K , Onorato J , Chen XQ , Abell LM , Lu H , Locke G , Caporuscio C , Adam LP , Gordon D , Wexler RR , Finlay HJ
Ref : Bioorganic & Medicinal Chemistry Lett , 29 :1918 , 2019
Abstract :
PubMedSearch : Kim_2019_Bioorg.Med.Chem.Lett_29_1918
PubMedID: 31176700
Gene_locus related to this paper: human-LIPG