Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM20724
Substrate
BDBM20717
Meas. Tech.
In Vitro FlashPlate Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
9±n/a nM
Citation
 Zhao, GSouers, AJVoorbach, MFalls, HDDroz, BBrodjian, SLau, YYIyengar, RRGao, JJudd, ASWagaw, SHRavn, MMEngstrom, KMLynch, JKMulhern, MMFreeman, JDayton, BDWang, XGrihalde, NFry, DBeno, DWMarsh, KCSu, ZDiaz, GJCollins, CASham, HReilly, RMBrune, MEKym, PR Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J Med Chem 51:380-3 (2008) [PubMed]  Article 
Target
Name:
Diacylglycerol O-acyltransferase 1
Synonyms:
ACAT-related gene product 1 | AGRP1 | Acyl coA-diacylglycerol acyl transferase 1 (DGAT1) | DGAT | DGAT1 | DGAT1_HUMAN | Diacylglycerol Acyltransferase (DGAT1) | Diacylglycerol O-acyltransferase 1 | Diacylglycerol O-acyltransferase 1 (DGAT1) | Diglyceride acyltransferase
Type:
Protein
Mol. Mass.:
55297.82
Organism:
Homo sapiens (Human)
Description:
O75907
Residue:
488
Sequence:
MGDRGSSRRRRTGSRPSSHGGGGPAAAEEEVRDAAAGPDVGAAGDAPAPAPNKDGDAGVGSGHWELRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQVVSLFLKDPYSWPAPCLVIAANVFAVAAFQVEKRLAVGALTEQAGLLLHVANLATILCFPAAVVLLVESITPVGSLLALMAHTILFLKLFSYRDVNSWCRRARAKAASAGKKASSAAAPHTVSYPDNLTYRDLYYFLFAPTLCYELNFPRSPRIRKRFLLRRILEMLFFTQLQVGLIQQWMVPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWLFHSCLNAVAELMQFGDREFYRDWWNSESVTYFWQNWNIPVHKWCIRHFYKPMLRRGSSKWMARTGVFLASAFFHEYLVSVPLRMFRLWAFTGMMAQIPLAWFVGRFFQGNYGNAAVWLSLIIGQPIAVLMYVHDYYVLNYEAPAAEA
  
Inhibitor
Name:
BDBM20724
Synonyms:
(1R,2R)-2-{[4-(4-{[(4-methoxyphenyl)carbamoyl]amino}phenyl)phenyl]carbonyl}cyclopentane-1-carboxylic acid | Urea-based Analogue, 4h
Type:
Small organic molecule
Emp. Form.:
C27H26N2O5
Mol. Mass.:
458.5057
SMILES:
COc1ccc(NC(=O)Nc2ccc(cc2)-c2ccc(cc2)C(=O)[C@@H]2CCC[C@H]2C(O)=O)cc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM20717
Synonyms:
(1-decanoyloxy-3-hydroxypropan-2-yl) decanoate | 1,2-didecanoyl-sn-glycerol | 1-(decanoyloxy)-3-hydroxypropan-2-yl decanoate | didecanoyl glycerol
Type:
n/a
Emp. Form.:
C23H44O5
Mol. Mass.:
400.5925
SMILES:
CCCCCCCCCC(=O)OCC(CO)OC(=O)CCCCCCCCC
Structure:
Search PDB for entries with ligand similarity: