Reaction Details |
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Target | Diacylglycerol O-acyltransferase 1 |
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Ligand | BDBM50239480 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1666099 (CHEMBL4015895) |
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IC50 | 151±n/a nM |
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Citation | Nakajima, K; Chatelain, R; Clairmont, KB; Commerford, R; Coppola, GM; Daniels, T; Forster, CJ; Gilmore, TA; Gong, Y; Jain, M; Kanter, A; Kwak, Y; Li, J; Meyers, CD; Neubert, AD; Szklennik, P; Tedesco, V; Thompson, J; Truong, D; Yang, Q; Hubbard, BK; Serrano-Wu, MH Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. J Med Chem60:4657-4664 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Diacylglycerol O-acyltransferase 1 |
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Name: | Diacylglycerol O-acyltransferase 1 |
Synonyms: | DGAT1_MOUSE | Dgat | Dgat1 | Diacyl Glycerolacyltransferase 1 (DGAT-1) | Diacylglycerol O-acyltransferase 1 (DGAT1) | Diglyceride acyltransferase |
Type: | Enzyme |
Mol. Mass.: | 56810.61 |
Organism: | Mus musculus (mouse) |
Description: | In this assay, recombinant mouse DGAT-1 containing an N-terminal His6-epitope tag was produced in the baculovirus expression system. |
Residue: | 498 |
Sequence: | MGDRGGAGSSRRRRTGSRVSVQGGSGPKVEEDEVRDAAVSPDLGAGGDAPAPAPAPAHTR
DKDGRTSVGDGYWDLRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKY
GILVDPIQVVSLFLKDPYSWPAPCVIIASNIFVVAAFQIEKRLAVGALTEQMGLLLHVVN
LATIICFPAAVALLVESITPVGSVFALASYSIMFLKLYSYRDVNLWCRQRRVKAKAVSTG
KKVSGAAAQQAVSYPDNLTYRDLYYFIFAPTLCYELNFPRSPRIRKRFLLRRVLEMLFFT
QLQVGLIQQWMVPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWFFHSCLNAV
AELLQFGDREFYRDWWNAESVTYFWQNWNIPVHKWCIRHFYKPMLRHGSSKWVARTGVFL
TSAFFHEYLVSVPLRMFRLWAFTAMMAQVPLAWIVGRFFQGNYGNAAVWVTLIIGQPVAV
LMYVHDYYVLNYDAPVGV
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BDBM50239480 |
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n/a |
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Name | BDBM50239480 |
Synonyms: | CHEMBL4074410 |
Type | Small organic molecule |
Emp. Form. | C29H28N4O4 |
Mol. Mass. | 496.557 |
SMILES | COc1ccc(cc1)-c1nnc(o1)-c1ccc2nc([nH]c2c1)-c1c(C)cc(CC(C)(C)C(O)=O)cc1C |
Structure |
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