Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM20718
Substrate
BDBM20717
Meas. Tech.
In Vitro FlashPlate Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
16±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:
DGAT1_MOUSE | Dgat | Dgat1 | Diacyl Glycerolacyltransferase 1 (DGAT-1) | Diacylglycerol O-acyltransferase 1 (DGAT1) | Diglyceride acyltransferase
Type:
Enzyme
Mol. Mass.:
56810.61
Organism:
Mus musculus (mouse)
Description:
In this assay, recombinant mouse DGAT-1 containing an N-terminal His6-epitope tag was produced in the baculovirus expression system.
Residue:
498
Sequence:
MGDRGGAGSSRRRRTGSRVSVQGGSGPKVEEDEVRDAAVSPDLGAGGDAPAPAPAPAHTRDKDGRTSVGDGYWDLRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQVVSLFLKDPYSWPAPCVIIASNIFVVAAFQIEKRLAVGALTEQMGLLLHVVNLATIICFPAAVALLVESITPVGSVFALASYSIMFLKLYSYRDVNLWCRQRRVKAKAVSTGKKVSGAAAQQAVSYPDNLTYRDLYYFIFAPTLCYELNFPRSPRIRKRFLLRRVLEMLFFTQLQVGLIQQWMVPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWFFHSCLNAVAELLQFGDREFYRDWWNAESVTYFWQNWNIPVHKWCIRHFYKPMLRHGSSKWVARTGVFLTSAFFHEYLVSVPLRMFRLWAFTAMMAQVPLAWIVGRFFQGNYGNAAVWVTLIIGQPVAVLMYVHDYYVLNYDAPVGV
  
Inhibitor
Name:
BDBM20718
Synonyms:
(1R,2R)-2-({4-[4-({[2-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]phenyl}carbonyl)cyclopentane-1-carboxylic acid | Urea-based Analogue, 4b
Type:
Small organic molecule
Emp. Form.:
C27H23F3N2O4
Mol. Mass.:
496.4777
SMILES:
OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2C(F)(F)F)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: