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Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM50341770
Substrate
n/a
Meas. Tech.
ChEMBL_743545 (CHEMBL1767986)
EC50
93±n/a nM
Citation
Qian, Y; Wertheimer, SJ; Ahmad, M; Cheung, AW; Firooznia, F; Hamilton, MM; Hayden, S; Li, S; Marcopulos, N; McDermott, L; Tan, J; Yun, W; Guo, L; Pamidimukkala, A; Chen, Y; Huang, KS; Ramsey, GB; Whittard, T; Conde-Knape, K; Taub, R; Rondinone, CM; Tilley, J; Bolin, D Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem 54:2433-46 (2011) [PubMed] Article
More Info.:
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:
BDBM50341770
Synonyms:
4-{5-[(2-Phenyl-5-trifluoromethyloxazole-4-carbonyl)-amino]pyridin-2-yl}piperazine-1-carboxylic Acid Ethyl Ester | CHEMBL1766888
Type:
Small organic molecule
Emp. Form.:
C23H22F3N5O4
Mol. Mass.:
489.4471
SMILES:
CCOC(=O)N1CCN(CC1)c1ccc(NC(=O)c2nc(oc2C(F)(F)F)-c2ccccc2)cn1