Reaction Details |
| Report a problem with these data |
Target | Diacylglycerol O-acyltransferase 1 |
---|
Ligand | BDBM27951 |
---|
Substrate/Competitor | BDBM27948 |
---|
Meas. Tech. | DGAT Enzyme Inhibition Assay |
---|
pH | 7.4±n/a |
---|
Temperature | 295.15±n/a K |
---|
IC50 | 28±n/a nM |
---|
Citation | Birch, AM; Birtles, S; Buckett, LK; Kemmitt, PD; Smith, GJ; Smith, TJ; Turnbull, AV; Wang, 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
|
|
|
BDBM27951 |
---|
BDBM27948 |
---|
Name | BDBM27951 |
Synonyms: | 2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl}phenyl)bicyclo[2.2.2]octan-1-yl]propanoic acid | bicyclo[2.2.2]octane-pyrimido[4,5-b][1,4]oxazine deriv., 5 |
Type | Small organic molecule |
Emp. Form. | C25H30N4O3 |
Mol. Mass. | 434.5307 |
SMILES | CC(C(O)=O)C12CCC(CC1)(CC2)c1ccc(cc1)C1=Nc2c(N)ncnc2OC1(C)C |t:22| |
Structure |
|