Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM435241
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
100±n/a nM
Citation
 Imbriglio, JLiang, RLondon, CMarby, KTata, JYou, MXiong, 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:
BDBM435241
Synonyms:
8-(((trans)-2-(3-methyl-1,2,4- oxadiazol-5-yl) cyclopropanecarboxamido)methyl)-N- (pyridin-3-yl)-5-(3-(trifluoromethyl) phenyl)-3,4-dihydroisoquinoline- 2(1H)-carboxamide (mixture of 2 isomers) | US10568876, Example 6
Type:
Small organic molecule
Emp. Form.:
C31H29N9O3
Mol. Mass.:
575.6205
SMILES:
Cc1noc(n1)[C@H]1C[C@@H]1C(=O)NCc1ccc(-c2cccc(c2)-n2ccnn2)c2CCN(Cc12)C(=O)Nc1cccnc1 |r|
Structure:
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