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Assay Detail

CHEMBL5142292

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of 125I-labeled angiotensin I from from human plasma renin by gamma counter based competitive radioimmunoassay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor.
Iijima D, Sugama H, Takahashi Y, Hirai M, Togashi Y, Xie J, Shen J, Ke Y, Akatsuka H, Kawaguchi T, Takedomi K, Kashima A, Nishio M, Inui Y, Yoneda H, Xia G, Iijima T.
J Med Chem (2022) 65 : 10882 -10897
PubMed 35939295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.13 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4110551 SITOKIREN 3.0 1 9.35
CHEMBL5174310 1 9.15
CHEMBL4114302 1 8.85
CHEMBL5187830 1 8.74
CHEMBL5200104 1 8.59
CHEMBL5188936 1 8.19
CHEMBL5176170 1 7.72
CHEMBL5190224 1 7.48
CHEMBL3699637 1 7.08
CHEMBL5184827 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4110551 SITOKIREN IC50 = 0.45 nM 9.35
CHEMBL5174310 IC50 = 0.7 nM 9.15
CHEMBL4114302 IC50 = 1.4 nM 8.85
CHEMBL5187830 IC50 = 1.8 nM 8.74
CHEMBL5200104 IC50 = 2.6 nM 8.59
CHEMBL5188936 IC50 = 6.5 nM 8.19
CHEMBL5176170 IC50 = 19.0 nM 7.72
CHEMBL5190224 IC50 = 33.0 nM 7.48
CHEMBL3699637 IC50 = 84.0 nM 7.08
CHEMBL5184827 IC50 = 661.0 nM 6.18