Reaction Details Report a problem with these data
Target
Diacylglycerol O-acyltransferase 2
Ligand
BDBM276754
Substrate
n/a
Meas. Tech.
ChEMBL_2187623 (CHEMBL5099705)
IC50
196±n/a nM
Citation
 Futatsugi, K; Cabral, S; Kung, DW; Huard, K; Lee, E; Boehm, M; Bauman, J; Clark, RW; Coffey, SB; Crowley, C; Dechert-Schmitt, AM; Dowling, MS; Dullea, R; Gosset, JR; Kalgutkar, AS; Kou, K; Li, Q; Lian, Y; Loria, PM; Londregan, AT; Niosi, M; Orozco, C; Pettersen, JC; Pfefferkorn, JA; Polivkova, J; Ross, TT; Sharma, R; Stock, IA; Tesz, G; Wisniewska, H; Goodwin, B; Price, DA Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis. J Med Chem 65:15000-15013 (2022) [PubMed] 
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:
BDBM276754
Synonyms:
N-(1,1-dioxidotetrahydro- thiophen-3-yl)-2-(5-((3- ethoxypyridin-2-yl)oxy) pyridin-3-yl)pyrimidine- 5-carboxamide | US10071992, Example 3.3 | US11034678, Example 3.3 | US11065249, WO2018033832-Ex.-3.3 | WO2018033832, Ex. 3.3
Type:
Small organic molecule
Emp. Form.:
C21H21N5O5S
Mol. Mass.:
455.487
SMILES:
CCOc1cccnc1Oc1cncc(c1)-c1ncc(cn1)C(=O)NC1CCS(=O)(=O)C1
Structure:
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