Reaction Details |
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Target | Renin |
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Ligand | BDBM18012 |
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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 | 0.067±n/a nM |
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Citation | Holsworth, DD; Jalaie, M; Belliotti, T; Cai, C; Collard, W; Ferreira, S; Powell, NA; Stier, M; Zhang, E; McConnell, P; Mochalkin, I; Ryan, MJ; Bryant, J; Li, T; Kasani, A; Subedi, R; Maiti, SN; Edmunds, JJ Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors. Bioorg Med Chem Lett17:3575-80 (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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BDBM18012 |
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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: | |