Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50385406
Substrate
n/a
Meas. Tech.
ChEMBL_822962 (CHEMBL2038283)
IC50
540±n/a nM
Citation
 McCoull, WAddie, MSBirch, AMBirtles, SBuckett, LKButlin, RJBowker, SSBoyd, SChapman, SDavies, RDDonald, CSGreen, CPJenner, CKemmitt, PDLeach, AGMoody, GCGutierrez, PMNewcombe, NJNowak, TPacker, MJPlowright, ATRevill, JSchofield, PSheldon, CStokes, STurnbull, AVWang, SJWhalley, DPWood, JM Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorg Med Chem Lett 22:3873-8 (2012) [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:
BDBM50385406
Synonyms:
CHEMBL2036577
Type:
Small organic molecule
Emp. Form.:
C21H21FN6O3
Mol. Mass.:
424.4282
SMILES:
CC(=O)N1CCN(CC1)c1ccc(NC(=O)c2nnc(Nc3ccccc3F)o2)cc1
Structure:
Search PDB for entries with ligand similarity: