Reaction Details
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Target
Renin
Ligand
BDBM17965
Substrate
Green Flourescent Protein (tGFP)
Meas. Tech.
In Vitro Renin IC50 Determinations (Tandem GFP FRET Assay)
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
0.5±n/a nM
Citation
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Target
Name:
Renin
Synonyms:
Angiotensinogenase | REN | RENI_HUMAN
Type:
Enzyme
Mol. Mass.:
45058.99
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
406
Sequence:
MDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEWSQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRLYTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEMPALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGGQIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISGSTSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKKLCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR
Inhibitor
Name:
BDBM17965
Synonyms:
N-[2-(7-{[(2R)-1-(4-{3-[(2-methoxyphenyl)methoxy]propoxy}phenyl)piperazin-2-yl]methoxy}-1,2,3,4-tetrahydroquinolin-1-yl)ethyl]acetamide | Piperazine-based compound, 15
Type:
Small organic molecule
Emp. Form.:
C35H46N4O5
Mol. Mass.:
602.7635
SMILES:
COc1ccccc1COCCCOc1ccc(cc1)N1CCNC[C@@H]1COc1ccc2CCCN(CCNC(C)=O)c2c1 |r|
Substrate
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:
NA