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Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM435378
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
3343±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:
BDBM435378
Synonyms:
US10568876, Example 137 | methyl 3-(2-(4- methylcyclohexanecarbonyl)-8-((2- phenylcyclopropanecarboxamido)methyl)- 1,2,3,4-tetrahydroisoquinolin-5- yl)benzoate (mixture of 4 isomers)
Type:
Small organic molecule
Emp. Form.:
C36H40N2O4
Mol. Mass.:
564.7138
SMILES:
COC(=O)c1cccc(c1)-c1ccc(CNC(=O)C2CC2c2ccccc2)c2CN(CCc12)C(=O)C1CCC(C)CC1 |(-4.92,-4.9,;-3.59,-4.13,;-2.26,-4.9,;-2.26,-6.44,;-.92,-4.13,;.41,-4.9,;1.74,-4.13,;1.74,-2.59,;.41,-1.82,;-.92,-2.59,;.41,-.28,;1.74,.49,;1.74,2.03,;.41,2.8,;.41,4.34,;1.74,5.11,;3.08,4.34,;3.08,2.8,;4.41,5.11,;5.18,6.44,;5.95,5.11,;7.28,4.34,;7.68,2.85,;9.17,2.45,;10.26,3.54,;9.86,5.03,;8.37,5.43,;-.92,2.03,;-2.26,2.8,;-3.59,2.03,;-3.59,.49,;-2.26,-.28,;-.92,.49,;-4.92,2.8,;-4.92,4.34,;-6.26,2.03,;-7.59,2.8,;-8.93,2.03,;-8.93,.49,;-10.26,-.28,;-7.59,-.28,;-6.26,.49,)|
Structure:
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