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Assay Detail

CHEMBL1799739

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

Binding
Inhibition of human ERG
35
Total Activities
35
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

Publication

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S.
Bioorg Med Chem Lett (2011) 21 : 3970 -3975
PubMed 21621998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 5.11 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1796075 1 6.12
CHEMBL1761519 1 6.10
CHEMBL1796073 1 6.02
CHEMBL1796074 1 5.92
CHEMBL1796064 1 5.77
CHEMBL1795909 1 5.32
CHEMBL1796062 1 5.30
CHEMBL1795907 1 5.17
CHEMBL1795901 1 5.14
CHEMBL1795911 1 5.12
CHEMBL1795913 1 5.08
CHEMBL1796071 1 4.96
CHEMBL1795912 1 4.96
CHEMBL1796077 1 4.92
CHEMBL1795908 1 4.89
CHEMBL1796078 1 4.82
CHEMBL1795916 1 4.82
CHEMBL1795914 1 4.77
CHEMBL1796065 1 4.77
CHEMBL1796060 1 4.75
CHEMBL1796063 1 4.75
CHEMBL1796070 1 4.64
CHEMBL1796067 1 4.57
CHEMBL1795906 1 4.55
CHEMBL1795910 1 4.55
CHEMBL1795902 1 -
CHEMBL1795903 1 -
CHEMBL1795904 1 -
CHEMBL1795905 1 -
CHEMBL1796072 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1796075 Ki = 750.0 nM 6.12
CHEMBL1761519 Ki = 800.0 nM 6.10
CHEMBL1796073 Ki = 950.0 nM 6.02
CHEMBL1796074 Ki = 1200.0 nM 5.92
CHEMBL1796064 Ki = 1700.0 nM 5.77
CHEMBL1795909 Ki = 4800.0 nM 5.32
CHEMBL1796062 Ki = 5000.0 nM 5.30
CHEMBL1795907 Ki = 6800.0 nM 5.17
CHEMBL1795901 Ki = 7200.0 nM 5.14
CHEMBL1795911 Ki = 7600.0 nM 5.12
CHEMBL1795913 Ki = 8400.0 nM 5.08
CHEMBL1796071 Ki = 11000.0 nM 4.96
CHEMBL1795912 Ki = 11000.0 nM 4.96
CHEMBL1796077 Ki = 12000.0 nM 4.92
CHEMBL1795908 Ki = 13000.0 nM 4.89
CHEMBL1796078 Ki = 15000.0 nM 4.82
CHEMBL1795916 Ki = 15000.0 nM 4.82
CHEMBL1795914 Ki = 17000.0 nM 4.77
CHEMBL1796065 Ki = 17000.0 nM 4.77
CHEMBL1796060 Ki = 18000.0 nM 4.75
CHEMBL1796063 Ki = 18000.0 nM 4.75
CHEMBL1796070 Ki = 23000.0 nM 4.64
CHEMBL1796067 Ki = 27000.0 nM 4.57
CHEMBL1795906 Ki = 28000.0 nM 4.55
CHEMBL1795910 Ki = 28000.0 nM 4.55
CHEMBL1796061 Ki > 29000.0 nM -
CHEMBL1795915 Ki > 29000.0 nM -
CHEMBL1796066 Ki > 29000.0 nM -
CHEMBL1796068 Ki > 29000.0 nM -
CHEMBL1796069 Ki > 29000.0 nM -
CHEMBL1796072 Ki > 29000.0 nM -
CHEMBL1795905 Ki > 29000.0 nM -
CHEMBL1795904 Ki > 29000.0 nM -
CHEMBL1795903 Ki > 29000.0 nM -
CHEMBL1795902 Ki > 29000.0 nM -