| Reaction Details |
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 | Report a problem with these data |
| Target | Glycogen phosphorylase, liver form |
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| Ligand | BDBM27740 |
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| Substrate/Competitor | BDBM24362 |
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| Meas. Tech. | Human Liver GPa Enzymatic Activity Assay |
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| pH | 7.6±n/a |
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| Temperature | 298.15±n/a K |
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| IC50 | 13±7 nM |
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| Citation |  Thomson, SA; Banker, P; Bickett, DM; Boucheron, JA; Carter, HL; Clancy, DC; Cooper, JP; Dickerson, SH; Garrido, DM; Nolte, RT; Peat, AJ; Sheckler, LR; Sparks, SM; Tavares, FX; Wang, L; Wang, TY; Weiel, JE Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy. Bioorg Med Chem Lett19:1177-82 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| Glycogen phosphorylase, liver form |
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| Name: | Glycogen phosphorylase, liver form |
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| Synonyms: | Glycogen Phosphorylase (PYGL) | Glycogen Phosphorylase, liver form | Liver glycogen phosphorylase | PYGL | PYGL_HUMAN |
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| Type: | Homodimer |
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| Mol. Mass.: | 97153.98 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Dimers associate into a tetramer to form the enzymatically active phosphorylase A. |
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| Residue: | 847 |
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| Sequence: | MAKPLTDQEKRRQISIRGIVGVENVAELKKSFNRHLHFTLVKDRNVATTRDYYFALAHTV
RDHLVGRWIRTQQHYYDKCPKRVYYLSLEFYMGRTLQNTMINLGLQNACDEAIYQLGLDI
EELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEYGIFNQKIRDGWQVEEA
DDWLRYGNPWEKSRPEFMLPVHFYGKVEHTNTGTKWIDTQVVLALPYDTPVPGYMNNTVN
TMRLWSARAPNDFNLRDFNVGDYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFV
VAATLQDIIRRFKASKFGSTRGAGTVFDAFPDQVAIQLNDTHPALAIPELMRIFVDIEKL
PWSKAWELTQKTFAYTNHTVLPEALERWPVDLVEKLLPRHLEIIYEINQKHLDRIVALFP
KDVDRLRRMSLIEEEGSKRINMAHLCIVGSHAVNGVAKIHSDIVKTKVFKDFSELEPDKF
QNKTNGITPRRWLLLCNPGLAELIAEKIGEDYVKDLSQLTKLHSFLGDDVFLRELAKVKQ
ENKLKFSQFLETEYKVKINPSSMFDVQVKRIHEYKRQLLNCLHVITMYNRIKKDPKKLFV
PRTVIIGGKAAPGYHMAKMIIKLITSVADVVNNDPMVGSKLKVIFLENYRVSLAEKVIPA
TDLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENLFIFGMRIDDVA
ALDKKGYEAKEYYEALPELKLVIDQIDNGFFSPKQPDLFKDIINMLFYHDRFKVFADYEA
YVKCQDKVSQLYMNPKAWNTMVLKNIAASGKFSSDRTIKEYAQNIWNVEPSDLKISLSNE
SNKVNGN
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| BDBM27740 |
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| BDBM24362 |
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| Name | BDBM27740 |
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| Synonyms: | (2S)-2-cyclohexyl-2-{[2-({[4-(cyclopropylmethyl)-2,6-dimethylphenyl]carbamoyl}amino)-4-fluorophenyl]formamido}acetic acid | anthranilimide based compound, 16 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H34FN3O4 |
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| Mol. Mass. | 495.5857 |
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| SMILES | Cc1cc(CC2CC2)cc(C)c1NC(=O)Nc1cc(F)ccc1C(=O)N[C@@H](C1CCCCC1)C(O)=O |r| |
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| Structure | 
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