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Assay Detail

CHEMBL2155358

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Binding
Inhibition of cynomolgus monkey plasma renin activity after 60 mins by competitive RIA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca fascicularis
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Renin (CHEMBL2046264)
Type SINGLE PROTEIN
Organism Macaca fascicularis

Publication

Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.
Nakamura Y, Fujimoto T, Ogawa Y, Sugita C, Miyazaki S, Tamaki K, Takahashi M, Matsui Y, Nagayama T, Manabe K, Mizuno M, Masubuchi N, Chiba K, Nishi T.
ACS Med Chem Lett (2012) 3 : 754 -758
PubMed 24900544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.15 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152353 1 8.20
CHEMBL3545059 ALISKIREN FUMARATE 4.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152353 IC50 = 6.3 nM 8.20
CHEMBL3545059 ALISKIREN FUMARATE IC50 = 8.0 nM 8.10