Reaction Details Report a problem with these data
Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM486380
Substrate
n/a
Meas. Tech.
DGAT2 Enzymatic Activity Assay
IC50
78.0±n/a nM
Citation
 Shen, D; Graham, TH; Jiang, J; Ding, F; Tudge, C Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 US Patent  US10947222 Publication Date 3/16/2021 
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:
BDBM486380
Synonyms:
3-(2-chlorophenyl)-1-(5- fluoropyrimidin-2-yl)-N-(3-methyl-1,1- dioxidotetrahydrothiophen-3-yl)-1H- indole-6-carboxamide (enantiomer A, fast) | US10947222, Example 15-A
Type:
Small organic molecule
Emp. Form.:
C24H20ClFN4O3S
Mol. Mass.:
498.957
SMILES:
C[C@]1(CCS(=O)(=O)C1)NC(=O)c1ccc2c(cn(-c3ncc(F)cn3)c2c1)-c1ccccc1Cl |r|
Structure:
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