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Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM435345
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1841±n/a nM
Citation
 Imbriglio, J; Liang, R; London, C; Marby, K; Tata, J; You, M; Xiong, Y Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 US Patent  US10568876 Publication Date 2/25/2020 
Target
Name:
Diacylglycerol O-acyltransferase 2
Synonyms:
ARAT | Acyl-CoA retinol O-fatty-acyltransferase | DGAT2 | DGAT2_HUMAN | Diacylglycerol O-acyltransferase 2 (DGAT2) | Diglyceride acyltransferase 2 | Retinol O-fatty-acyltransferase
Type:
Multi-pass membrane protein
Mol. Mass.:
43848.90
Organism:
Homo sapiens (Human)
Description:
Q96PD7
Residue:
388
Sequence:
MKTLIAAYSGVLRGERQAEADRSQRSHGGPALSREGSGRWGTGSSILSALQDLFSVTWLNRSKVEKQLQVISVLQWVLSFLVLGVACSAILMYIFCTDCWLIAVLYFTWLVFDWNTPKKGGRRSQWVRNWAVWRYFRDYFPIQLVKTHNLLTTRNYIFGYHPHGIMGLGAFCNFSTEATEVSKKFPGIRPYLATLAGNFRMPVLREYLMSGGICPVSRDTIDYLLSKNGSGNAIIIVVGGAAESLSSMPGKNAVTLRNRKGFVKLALRHGADLVPIYSFGENEVYKQVIFEEGSWGRWVQKKFQKYIGFAPCIFHGRGLFSSDTWGLVPYSKPITTVVGEPITIPKLEHPTQQDIDLYHTMYMEALVKLFDKHKTKFGLPETEVLEVN
  
Inhibitor
Name:
BDBM435345
Synonyms:
(trans)-2-(3-methyl-1,2,4-oxadiazol-5-yl)- N-((2-((4-methylthiazol-5-yl)methyl)-5- (3-(trifluoromethoxy)phenyl)-1,2,3,4- tetrahydroisoquinolin-8- yl)methyl)cyclopropanecarboxamide (mixture of 2 isomers) | US10568876, Example 106
Type:
Small organic molecule
Emp. Form.:
C29H28F3N5O3S
Mol. Mass.:
583.625
SMILES:
Cc1noc(n1)[C@@H]1CC1C(=O)NCc1ccc(-c2cccc(OC(F)(F)F)c2)c2CCN(Cc3scnc3C)Cc12 |r|
Structure:
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