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Target
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
Ligand
BDBM38169
Substrate
n/a
Meas. Tech.
MGAT LCMS Assay
pH
7.4±n/a
IC50
27.0±n/a nM
Comments
extracted
Citation
 Ahmad, S Tetrazolone-substituted dihydropyridinone MGAT2 inhibitors US Patent  US10093650 Publication Date 10/9/2018 
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:
BDBM38169
Synonyms:
(S)-3-(5-Oxo-4,5-dihydro-1H-tetrazol-1-yl)-4-(p-tolyl)-6-(4-(4,4,4-trifluorobutoxy)phenyl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one | US10093650, Example 1 | US10329273, Example 1
Type:
Small organic molecule
Emp. Form.:
C32H31F6N5O5
Mol. Mass.:
679.6095
SMILES:
COc1ccc(Cn2nnn(CC(=O)NC(CC(=O)c3ccc(C)cc3)(c3ccc(OCCCC(F)(F)F)cc3)C(F)(F)F)c2=O)cc1
Structure:
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