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Assay Detail

CHEMBL861323

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

Binding
Inhibition of PKA at 5 uM ATP
5
Total Activities
5
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

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Zhu GD, Gong J, Claiborne A, Woods KW, Gandhi VB, Thomas S, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Stoll VS, De Jong R, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL.
Bioorg Med Chem Lett (2006) 16 : 3150 -3155
PubMed 16603355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.28 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207544 1 9.00
CHEMBL383264 1 8.68
CHEMBL378963 1 8.30
CHEMBL210390 1 8.10
CHEMBL210246 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207544 IC50 = 1.0 nM 9.00
CHEMBL383264 IC50 = 2.1 nM 8.68
CHEMBL378963 IC50 = 5.0 nM 8.30
CHEMBL210390 IC50 = 8.0 nM 8.10
CHEMBL210246 IC50 = 48.0 nM 7.32