| Reaction Details |
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 | Report a problem with these data |
| Target | Diacylglycerol O-acyltransferase 1 |
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| Ligand | BDBM20716 |
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| Substrate/Competitor | BDBM20717 |
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| Meas. Tech. | In Vitro FlashPlate Assay |
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| pH | 7.5±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 24±n/a nM |
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| Citation |  Zhao, G; Souers, AJ; Voorbach, M; Falls, HD; Droz, B; Brodjian, S; Lau, YY; Iyengar, RR; Gao, J; Judd, AS; Wagaw, SH; Ravn, MM; Engstrom, KM; Lynch, JK; Mulhern, MM; Freeman, J; Dayton, BD; Wang, X; Grihalde, N; Fry, D; Beno, DW; Marsh, KC; Su, Z; Diaz, GJ; Collins, CA; Sham, H; Reilly, RM; Brune, ME; Kym, PR Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J Med Chem51:380-3 (2008) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Diacylglycerol O-acyltransferase 1 |
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| Name: | Diacylglycerol O-acyltransferase 1 |
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| Synonyms: | DGAT1_MOUSE | Dgat | Dgat1 | Diacyl Glycerolacyltransferase 1 (DGAT-1) | Diacylglycerol O-acyltransferase 1 (DGAT1) | Diglyceride acyltransferase |
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| Type: | Enzyme |
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| Mol. Mass.: | 56810.61 |
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| Organism: | Mus musculus (mouse) |
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| Description: | In this assay, recombinant mouse DGAT-1 containing an N-terminal His6-epitope tag was produced in the baculovirus expression system. |
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| Residue: | 498 |
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| Sequence: | MGDRGGAGSSRRRRTGSRVSVQGGSGPKVEEDEVRDAAVSPDLGAGGDAPAPAPAPAHTR
DKDGRTSVGDGYWDLRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKY
GILVDPIQVVSLFLKDPYSWPAPCVIIASNIFVVAAFQIEKRLAVGALTEQMGLLLHVVN
LATIICFPAAVALLVESITPVGSVFALASYSIMFLKLYSYRDVNLWCRQRRVKAKAVSTG
KKVSGAAAQQAVSYPDNLTYRDLYYFIFAPTLCYELNFPRSPRIRKRFLLRRVLEMLFFT
QLQVGLIQQWMVPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWFFHSCLNAV
AELLQFGDREFYRDWWNAESVTYFWQNWNIPVHKWCIRHFYKPMLRHGSSKWVARTGVFL
TSAFFHEYLVSVPLRMFRLWAFTAMMAQVPLAWIVGRFFQGNYGNAAVWVTLIIGQPVAV
LMYVHDYYVLNYDAPVGV
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| BDBM20716 |
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| BDBM20717 |
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| Name | BDBM20716 |
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| Synonyms: | (1R,2R)-2-[(4-{4-[(phenylcarbamoyl)amino]phenyl}phenyl)carbonyl]cyclopentane-1-carboxylic acid | Urea-based Analogue, 4a |
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| Type | Small organic molecule |
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| Emp. Form. | C26H24N2O4 |
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| Mol. Mass. | 428.4798 |
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| SMILES | OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1 |r| |
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| Structure | 
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