Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50385436
Substrate
n/a
Meas. Tech.
ChEMBL_822962 (CHEMBL2038283)
IC50
210±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:
BDBM50385436
Synonyms:
CHEMBL2036741
Type:
Small organic molecule
Emp. Form.:
C22H15FN4O4
Mol. Mass.:
418.3773
SMILES:
OC(=O)c1ccc(cc1)-c1ccc(NC(=O)c2nnc(Nc3ccccc3F)o2)cc1
Structure:
Search PDB for entries with ligand similarity: