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Target
Diacylglycerol O-acyltransferase 1
Ligand
BDBM27947
Substrate
n/a
Meas. Tech.
ChEMBL_803191 (CHEMBL1954902)
IC50
16±n/a nM
Citation
 Dow, RL; Li, JC; Pence, MP; Gibbs, EM; LaPerle, JL; Litchfield, J; Piotrowski, DW; Munchhof, MJ; Manion, TB; Zavadoski, WJ; Walker, GS; McPherson, RK; Tapley, S; Sugarman, E; Guzman-Perez, A; DaSilva-Jardine, P Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. ACS Med Chem Lett 2:407-412 (2011) [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:
BDBM27947
Synonyms:
2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl}phenyl)cyclohexyl]acetic acid | pyrimido[4,5-b][1,4]oxazine derivative, 2
Type:
Small organic molecule
Emp. Form.:
C22H26N4O3
Mol. Mass.:
394.4668
SMILES:
CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1 |r,wU:19.21,wD:22.25,c:12,(1.74,.99,;.97,2.32,;2.46,2.72,;-.37,1.55,;-1.7,2.32,;-3.03,1.55,;-4.37,2.32,;-4.37,3.86,;-3.03,4.63,;-3.03,6.17,;-1.7,3.86,;-.37,4.63,;.97,3.86,;2.3,4.63,;2.3,6.17,;3.63,6.94,;4.97,6.17,;4.97,4.63,;3.63,3.86,;6.19,6.75,;6.19,8.3,;7.53,9.07,;8.86,8.3,;10.19,9.07,;11.53,8.3,;12.86,9.07,;11.53,6.76,;8.86,6.75,;7.53,5.98,)|
Structure:
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