Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50003735
Substrate
n/a
Meas. Tech.
ChEMBL_1336096 (CHEMBL3240807)
IC50
90±n/a nM
Citation
 Fox, BMSugimoto, KIio, KYoshida, AZhang, JKLi, KHao, XLabelle, MSmith, MLRubenstein, SMYe, GMcMinn, DJackson, SChoi, RShan, BMa, JMiao, SMatsui, TOgawa, NSuzuki, MKobayashi, AOzeki, HOkuma, CIshii, YTomimoto, DFurakawa, NTanaka, MMatsushita, MTakahashi, MInaba, TSagawa, SKayser, F Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents. J Med Chem 57:3464-83 (2014) [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:
BDBM50003735
Synonyms:
CHEMBL3235301
Type:
Small organic molecule
Emp. Form.:
C17H20N4O
Mol. Mass.:
296.3669
SMILES:
CC(C)c1ccc(cc1)C1=Nc2c(N)ncnc2OC1(C)C |t:10|
Structure:
Search PDB for entries with ligand similarity: