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Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50362666
Substrate
n/a
Meas. Tech.
ChEMBL_797435 (CHEMBL1943098)
IC50
125±n/a nM
Citation
 Bali, U; Barba, O; Dawson, G; Gattrell, WT; Horswill, JG; Pan, DA; Procter, MJ; Rasamison, CM; Sambrook Smith, CP; Taylor-Warne, A; Wong-Kai-In, P Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability. Bioorg Med Chem Lett 22:824-8 (2012) [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:
BDBM50362666
Synonyms:
CHEMBL1939628
Type:
Small organic molecule
Emp. Form.:
C28H26N2O4
Mol. Mass.:
454.517
SMILES:
Cc1cc(NC(=O)c2ccc3ccccc3c2)ccc1-c1ccc(OCC(C)(C)C(O)=O)nc1
Structure:
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