Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50003732
Substrate
n/a
Meas. Tech.
ChEMBL_1336096 (CHEMBL3240807)
IC50
160±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:
BDBM50003732
Synonyms:
CHEMBL3235298
Type:
Small organic molecule
Emp. Form.:
C16H18N4O
Mol. Mass.:
282.3403
SMILES:
CCc1ccc(cc1)C1=Nc2c(N)ncnc2OC1(C)C |t:9|
Structure:
Search PDB for entries with ligand similarity: