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TargetDiacylglycerol O-acyltransferase 1
LigandBDBM27953
Substrate/CompetitorBDBM27948
Meas. Tech.DGAT Enzyme Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
IC50 120±n/a nM
Citation Birch, AMBirtles, SBuckett, LKKemmitt, PDSmith, GJSmith, TJTurnbull, AVWang, SJ Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem52:1558-68 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Diacylglycerol O-acyltransferase 1
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:
MGDRGSSRRRRTGSRPSSHGGGGPAAAEEEVRDAAAGPDVGAAGDAPAPAPNKDGDAGVG
SGHWELRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQV
VSLFLKDPYSWPAPCLVIAANVFAVAAFQVEKRLAVGALTEQAGLLLHVANLATILCFPA
AVVLLVESITPVGSLLALMAHTILFLKLFSYRDVNSWCRRARAKAASAGKKASSAAAPHT
VSYPDNLTYRDLYYFLFAPTLCYELNFPRSPRIRKRFLLRRILEMLFFTQLQVGLIQQWM
VPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWLFHSCLNAVAELMQFGDREF
YRDWWNSESVTYFWQNWNIPVHKWCIRHFYKPMLRRGSSKWMARTGVFLASAFFHEYLVS
VPLRMFRLWAFTGMMAQIPLAWFVGRFFQGNYGNAAVWLSLIIGQPIAVLMYVHDYYVLN
YEAPAAEA
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  Blast E-value cutoff:
BDBM27953
BDBM27948
NameBDBM27953
Synonyms:2-[3-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl}phenyl)adamantan-1-yl]acetic acid | adamantane-pyrimido[4,5-b][1,4]oxazine deriv., 7
TypeSmall organic molecule
Emp. Form.C26H30N4O3
Mol. Mass.446.5414
SMILESCC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)C12CC3CC(CC(CC(O)=O)(C3)C1)C2 |c:12,TLB:30:21:32:31.25.24,30:25:32:20.21.22,26:25:20:32.22.23,THB:24:25:20:32.22.23,24:23:20:31.30.25|
Structure
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