Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50239485
Substrate
n/a
Meas. Tech.
ChEMBL_1666098 (CHEMBL4015894)
IC50
132±n/a nM
Citation
 Nakajima, KChatelain, RClairmont, KBCommerford, RCoppola, GMDaniels, TForster, CJGilmore, TAGong, YJain, MKanter, AKwak, YLi, JMeyers, CDNeubert, ADSzklennik, PTedesco, VThompson, JTruong, DYang, QHubbard, BKSerrano-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:
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:
BDBM50239485
Synonyms:
CHEMBL4060245
Type:
Small organic molecule
Emp. Form.:
C22H12Cl3N3O
Mol. Mass.:
440.709
SMILES:
Clc1ccc(cc1)-c1cnc(o1)-c1ccc2nc([nH]c2c1)-c1c(Cl)cccc1Cl
Structure:
Search PDB for entries with ligand similarity: