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Assay Detail

CHEMBL5149786

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

Binding
Inhibition of human recombinant renin using sheep recombinant angiotensinogen substrate incubated for 1 hr by EIA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.
Iijima D, Sugama H, Awai N, Takahashi Y, Togashi Y, Takebe T, Xie J, Shen J, Ke Y, Akatsuka H, Kawaguchi T, Takedomi K, Kashima A, Nishio M, Inui Y, Yoneda H, Xia G, Iijima T.
ACS Med Chem Lett (2022) 13 : 1351 -1357
PubMed 35978678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.21 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5181888 1 6.11
CHEMBL5199179 1 4.92
CHEMBL5205574 1 4.60
CHEMBL5185263 1 -
CHEMBL5186347 1 -
CHEMBL5177567 1 -
CHEMBL5187637 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5181888 IC50 = 770.0 nM 6.11
CHEMBL5199179 IC50 = 12000.0 nM 4.92
CHEMBL5205574 IC50 = 25000.0 nM 4.60
CHEMBL5185263 IC50 > 30000.0 nM -
CHEMBL5186347 IC50 > 30000.0 nM -
CHEMBL5177567 IC50 - -
CHEMBL5187637 IC50 - -