Reaction Details |
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Target | Renin |
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Ligand | BDBM17989 |
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Substrate/Competitor | Green Flourescent Protein (tGFP) |
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Meas. Tech. | In Vitro Renin IC50 Determinations (Tandem GFP FRET Assay) |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1±n/a nM |
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Citation | Powell, NA; Ciske, FL; Cai, C; Holsworth, DD; Mennen, K; Van Huis, CA; Jalaie, M; Day, J; Mastronardi, M; McConnell, P; Mochalkin, I; Zhang, E; Ryan, MJ; Bryant, J; Collard, W; Ferreira, S; Gu, C; Collins, R; Edmunds, JJ Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. Bioorg Med Chem15:5912-49 (2007) [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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Renin |
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Name: | Renin |
Synonyms: | Angiotensinogenase | REN | RENI_HUMAN |
Type: | Enzyme |
Mol. Mass.: | 45058.99 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 406 |
Sequence: | MDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEW
SQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRL
YTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEM
PALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGG
QIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISG
STSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKK
LCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR
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BDBM17989 |
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Green Flourescent Protein (tGFP) |
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Name: | Green Flourescent Protein (tGFP) |
Synonyms: | n/a |
Type: | Other Protein Type |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | The tGFP substrate contained a nine amino acid (Ile-His-Pro-Phe-His-Leu-Val-Ile-His) recognition sequence for human renin flanked by two GPF proteins (W1B and Topaz). |
Residue: | 3 |
Sequence: | |