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Assay Detail

CHEMBL864414

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Binding
Inhibition of PKA at 10 uM ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

cAMP-dependent protein kinase (PKA) (CHEMBL2094138)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.
Bioorg Med Chem Lett (2006) 16 : 2000 -2007
PubMed 16413780 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.18 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL383264 1 8.68
CHEMBL388978 STAUROSPORINE 1 8.44
CHEMBL383541 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL383264 IC50 = 2.1 nM 8.68
CHEMBL388978 STAUROSPORINE IC50 = 3.6 nM 8.44
CHEMBL383541 IC50 = 38.0 nM 7.42