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Assay Detail

CHEMBL919347

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Binding
Inhibition of PKA by radiometric filter binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.
Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.
J Med Chem (2007) 50 : 2289 -2292
PubMed 17451235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.57 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228042 1 7.82
CHEMBL228133 1 7.48
CHEMBL104264 1 7.14
CHEMBL227381 1 6.77
CHEMBL227605 1 6.21
CHEMBL376388 1 5.28
CHEMBL375509 1 5.26
CHEMBL226712 1 -
CHEMBL389176 1 -
CHEMBL227998 1 -
CHEMBL227727 1 -
CHEMBL389685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228042 IC50 = 15.0 nM 7.82
CHEMBL228133 IC50 = 33.0 nM 7.48
CHEMBL104264 IC50 = 73.0 nM 7.14
CHEMBL227381 IC50 = 170.0 nM 6.77
CHEMBL227605 IC50 = 610.0 nM 6.21
CHEMBL376388 IC50 = 5200.0 nM 5.28
CHEMBL375509 IC50 = 5500.0 nM 5.26
CHEMBL226712 IC50 - -
CHEMBL389176 IC50 - -
CHEMBL227998 IC50 - -
CHEMBL227727 IC50 - -
CHEMBL389685 IC50 - -