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Target
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
Ligand
BDBM253649
Substrate
n/a
Meas. Tech.
MGAT LCMS Assay
pH
7.4±n/a
IC50
1.50±n/a nM
Comments
extracted
Citation
 Meng, W; Zhao, G Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders US Patent  US9701672 Publication Date 7/11/2017 
Target
Name:
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
Synonyms:
2.4.1.143 | Beta-1,2-N-acetylglucosaminyltransferase II | GNT-II | GlcNAc-T II | MGAT2 | MGAT2_HUMAN | Mannoside acetylglucosaminyltransferase 2 | Monoacylglycerol acyltransferase 2 (MGAT2) | Monoacylglycerol acyltransferase type 2 (h-MGAT2) | N-glycosyl-oligosaccharide-glycoprotein N-acetylglucosaminyltransferase II | h-MGAT2 (human monoacylglycerol acyltransferase type 2)
Type:
n/a
Mol. Mass.:
51567.80
Organism:
Homo sapiens (Human)
Description:
Q10469
Residue:
447
Sequence:
MRFRIYKRKVLILTLVVAACGFVLWSSNGRQRKNEALAPPLLDAEPARGAGGRGGDHPSVAVGIRRVSNVSAASLVPAVPQPEADNLTLRYRSLVYQLNFDQTLRNVDKAGTWAPRELVLVVQVHNRPEYLRLLLDSLRKAQGIDNVLVIFSHDFWSTEINQLIAGVNFCPVLQVFFPFSIQLYPNEFPGSDPRDCPRDLPKNAALKLGCINAEYPDSFGHYREAKFSQTKHHWWWKLHFVWERVKILRDYAGLILFLEEDHYLAPDFYHVFKKMWKLKQQECPECDVLSLGTYSASRSFYGMADKVDVKTWKSTEHNMGLALTRNAYQKLIECTDTFCTYDDYNWDWTLQYLTVSCLPKFWKVLVPQIPRIFHAGDCGMHHKKTCRPSTQSAQIESLLNNNKQYMFPETLTISEKFTVVAISPPRKNGGWGDIRDHELCKSYRRLQ
  
Inhibitor
Name:
BDBM253649
Synonyms:
(S)—N-(4-(5-Ethylthiophen-2-yl)-2-oxo-6-(4-((6,6,6-trifluorohexyl)oxy)phenyl)-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridin-3-yl)-2-(methylsulfonyl)acetamide | US9701672, 75
Type:
Small organic molecule
Emp. Form.:
C27H30F6N2O5S2
Mol. Mass.:
640.658
SMILES:
CCc1ccc(s1)C1=C(NC(=O)CS(C)(=O)=O)C(=O)N[C@@](C1)(c1ccc(OCCCCCC(F)(F)F)cc1)C(F)(F)F |r,c:8|
Structure:
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