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Assay Detail

CHEMBL889249

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Binding
Inhibition of PKA
6
Total Activities
6
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

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.
Zhu GD, Gandhi VB, Gong J, Thomas S, Woods KW, Song X, Li T, Diebold RB, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Bouska J, Olson A, Marsh KC, Stoll VS, Mamo M, Polakowski J, Campbell TJ, Martin RL, Gintant GA, Penning TD, Li Q, Rosenberg SH, Giranda VL.
J Med Chem (2007) 50 : 2990 -3003
PubMed 17523610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.89 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226625 1 8.30
CHEMBL427422 1 8.15
CHEMBL438483 1 8.05
CHEMBL226898 1 7.89
CHEMBL388312 1 7.82
CHEMBL226850 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226625 IC50 = 5.0 nM 8.30
CHEMBL427422 IC50 = 7.0 nM 8.15
CHEMBL438483 IC50 = 9.0 nM 8.05
CHEMBL226898 IC50 = 13.0 nM 7.89
CHEMBL388312 IC50 = 15.0 nM 7.82
CHEMBL226850 IC50 = 78.0 nM 7.11