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Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50239482
Substrate
n/a
Meas. Tech.
ChEMBL_1666099 (CHEMBL4015895)
IC50
913±n/a nM
Citation
 Nakajima, K; Chatelain, R; Clairmont, KB; Commerford, R; Coppola, GM; Daniels, T; Forster, CJ; Gilmore, TA; Gong, Y; Jain, M; Kanter, A; Kwak, Y; Li, J; Meyers, CD; Neubert, AD; Szklennik, P; Tedesco, V; Thompson, J; Truong, D; Yang, Q; Hubbard, BK; Serrano-Wu, MH Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. J Med Chem 60:4657-4664 (2017) [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:
BDBM50239482
Synonyms:
CHEMBL1683001
Type:
Small organic molecule
Emp. Form.:
C28H24N4O3
Mol. Mass.:
464.5152
SMILES:
Cc1cc(CCC(O)=O)cc(C)c1-c1nc2ccc(cc2[nH]1)C(=O)Nc1ccc2ccccc2n1
Structure:
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