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Assay Detail

CHEMBL801669

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

Functional
Inhibitory activity against human plasma renin at pH 7.4
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Rosenberg SH, Woods KW, Sham HL, Kleinert HD, Martin DL, Stein H, Cohen J, Egan DA, Bopp B, Merits I.
J Med Chem (1990) 33 : 1962 -1969
PubMed 2194033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.13 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58263 1 9.24
CHEMBL299055 1 8.96
CHEMBL345043 1 8.89
CHEMBL303076 1 8.82
CHEMBL61420 1 8.60
CHEMBL59135 1 8.14
CHEMBL61428 1 8.06
CHEMBL61777 1 8.02
CHEMBL58968 1 8.00
CHEMBL59887 1 7.96
CHEMBL300337 ENALKIREN 2.0 1 7.85
CHEMBL58859 1 7.85
CHEMBL305162 1 7.58
CHEMBL59236 1 7.57
CHEMBL58351 1 7.34
CHEMBL294379 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58263 IC50 = 0.57 nM 9.24
CHEMBL299055 IC50 = 1.1 nM 8.96
CHEMBL345043 IC50 = 1.3 nM 8.89
CHEMBL303076 IC50 = 1.5 nM 8.82
CHEMBL61420 IC50 = 2.5 nM 8.60
CHEMBL59135 IC50 = 7.3 nM 8.14
CHEMBL61428 IC50 = 8.7 nM 8.06
CHEMBL61777 IC50 = 9.6 nM 8.02
CHEMBL58968 IC50 = 9.9 nM 8.00
CHEMBL59887 IC50 = 11.0 nM 7.96
CHEMBL300337 ENALKIREN IC50 = 14.0 nM 7.85
CHEMBL58859 IC50 = 14.0 nM 7.85
CHEMBL305162 IC50 = 26.0 nM 7.58
CHEMBL59236 IC50 = 27.0 nM 7.57
CHEMBL58351 IC50 = 46.0 nM 7.34
CHEMBL294379 IC50 = 59.0 nM 7.23