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Assay Detail

CHEMBL861320

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

Binding
Inhibition of Akt1 at 5 uM ATP
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
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 28 7.21 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207544 1 9.10
CHEMBL378843 1 8.82
CHEMBL378963 1 8.74
CHEMBL209513 1 8.70
CHEMBL383264 1 8.70
CHEMBL210390 1 8.47
CHEMBL210246 1 8.46
CHEMBL379209 1 8.34
CHEMBL210089 1 7.92
CHEMBL380196 1 7.82
CHEMBL377764 1 7.66
CHEMBL378211 1 7.25
CHEMBL210333 1 7.24
CHEMBL378116 1 7.08
CHEMBL209564 1 6.91
CHEMBL206924 1 6.84
CHEMBL208962 1 6.80
CHEMBL378714 1 6.75
CHEMBL210093 1 6.64
CHEMBL210544 1 6.52
CHEMBL210783 1 6.39
CHEMBL381273 1 6.19
CHEMBL210628 1 6.16
CHEMBL208014 1 6.11
CHEMBL208961 1 6.00
CHEMBL207545 1 5.91
CHEMBL207215 1 5.91
CHEMBL210337 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207544 IC50 = 0.8 nM 9.10
CHEMBL378843 IC50 = 1.5 nM 8.82
CHEMBL378963 IC50 = 1.8 nM 8.74
CHEMBL209513 IC50 = 2.0 nM 8.70
CHEMBL383264 IC50 = 2.0 nM 8.70
CHEMBL210390 IC50 = 3.4 nM 8.47
CHEMBL210246 IC50 = 3.5 nM 8.46
CHEMBL379209 IC50 = 4.6 nM 8.34
CHEMBL210089 IC50 = 12.0 nM 7.92
CHEMBL380196 IC50 = 15.0 nM 7.82
CHEMBL377764 IC50 = 22.0 nM 7.66
CHEMBL378211 IC50 = 56.0 nM 7.25
CHEMBL210333 IC50 = 57.0 nM 7.24
CHEMBL378116 IC50 = 84.0 nM 7.08
CHEMBL209564 IC50 = 122.0 nM 6.91
CHEMBL206924 IC50 = 144.0 nM 6.84
CHEMBL208962 IC50 = 160.0 nM 6.80
CHEMBL378714 IC50 = 180.0 nM 6.75
CHEMBL210093 IC50 = 227.0 nM 6.64
CHEMBL210544 IC50 = 305.0 nM 6.52
CHEMBL210783 IC50 = 407.0 nM 6.39
CHEMBL381273 IC50 = 640.0 nM 6.19
CHEMBL210628 IC50 = 697.0 nM 6.16
CHEMBL208014 IC50 = 778.0 nM 6.11
CHEMBL208961 IC50 = 995.0 nM 6.00
CHEMBL207545 IC50 = 1240.0 nM 5.91
CHEMBL207215 IC50 = 1240.0 nM 5.91
CHEMBL210337 IC50 = 39500.0 nM 4.40