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Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50239480
Substrate
n/a
Meas. Tech.
ChEMBL_1666099 (CHEMBL4015895)
IC50
151±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:
Diacylglycerol O-acyltransferase 1 (DGAT1) | Diacyl Glycerolacyltransferase 1 (DGAT-1) | Diglyceride acyltransferase | DGAT1_MOUSE | Dgat1 | Dgat
Type:
Enzyme
Mol. Mass.:
56810.61
Organism:
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:
BDBM50239480
Synonyms:
CHEMBL4074410
Type:
Small organic molecule
Emp. Form.:
C29H28N4O4
Mol. Mass.:
496.21
SMILES:
COc1ccc(cc1)-c1nnc(o1)-c1ccc2nc([nH]c2c1)-c1c(C)cc(CC(C)(C)C(O)=O)cc1C
Structure:
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