Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM435237
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
112±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:
BDBM435237
Synonyms:
N-(isoxazol-3-yl)-8-(((trans)-2-(3- methyl-1,2,4-oxadiazol-5- yl)cyclopropanecarboxamido)methyl)- 5-(3-(trifluoromethoxy)phenyl)-3,4- dihydroisoquinoline-2(1H)- carboxamide (mixture of 2 isomers) | US10568876, Example 2
Type:
Small organic molecule
Emp. Form.:
C28H25F3N6O5
Mol. Mass.:
582.5305
SMILES:
Cc1noc(n1)[C@@H]1C[C@H]1C(=O)NCc1ccc(-c2cccc(OC(F)(F)F)c2)c2CCN(Cc12)C(=O)Nc1ccon1 |r|
Structure:
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