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Target
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
Ligand
BDBM201365
Substrate
n/a
Meas. Tech.
MGAT SPA Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
20±n/a nM
Comments
extracted
Citation
 Turdi, H; Hangeland, JJ; Lawrence, RM; Cheng, D; Ahmad, S; Meng, W; Brigance, RP; Devasthale, P; Zhao, G Aryl dihydropyridinones and piperidinone MGAT2 inhibitors US Patent  US9187424 Publication Date 11/17/2015 
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:
BDBM201365
Synonyms:
US9187424, 130
Type:
Small organic molecule
Emp. Form.:
C26H21F6N3O4
Mol. Mass.:
553.4531
SMILES:
Cc1ccc(cc1)C1=C(C(=O)Nc2ccno2)C(=O)NC(C1)(c1ccc(OCCC(F)(F)F)cc1)C(F)(F)F |c:8|
Structure:
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