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Assay Detail

CHEMBL867719

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Binding
Inhibition of Akt1 using 10 uM ATP
46
Total Activities
46
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

Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Li Q, Li T, Zhu GD, Gong J, Claibone A, Dalton C, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Bauch JL, Marsh KC, Bouska JJ, Arries S, De Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.
Bioorg Med Chem Lett (2006) 16 : 1679 -1685
PubMed 16403626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.08 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.82
CHEMBL203624 1 8.01
CHEMBL383541 1 7.85
CHEMBL203384 1 7.72
CHEMBL379914 1 7.64
CHEMBL203275 1 7.16
CHEMBL381703 1 7.10
CHEMBL381075 1 6.92
CHEMBL206183 1 6.85
CHEMBL381328 1 6.84
CHEMBL381610 1 6.83
CHEMBL382914 1 6.79
CHEMBL202787 1 6.75
CHEMBL203329 1 6.70
CHEMBL205415 1 6.56
CHEMBL206198 1 6.56
CHEMBL383254 1 6.55
CHEMBL205410 1 6.50
CHEMBL205871 1 6.49
CHEMBL381808 1 6.44
CHEMBL204012 1 6.30
CHEMBL383527 1 6.17
CHEMBL203673 1 6.16
CHEMBL202937 1 6.12
CHEMBL203685 1 6.06
CHEMBL202893 1 5.96
CHEMBL377294 1 5.57
CHEMBL381260 1 5.51
CHEMBL205514 1 5.50
CHEMBL206708 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 1.5 nM 8.82
CHEMBL203624 IC50 = 9.7 nM 8.01
CHEMBL383541 IC50 = 14.0 nM 7.85
CHEMBL203384 IC50 = 19.0 nM 7.72
CHEMBL379914 IC50 = 23.0 nM 7.64
CHEMBL203275 IC50 = 69.0 nM 7.16
CHEMBL381703 IC50 = 79.0 nM 7.10
CHEMBL381075 IC50 = 121.0 nM 6.92
CHEMBL206183 IC50 = 142.0 nM 6.85
CHEMBL381328 IC50 = 146.0 nM 6.84
CHEMBL381610 IC50 = 147.0 nM 6.83
CHEMBL382914 IC50 = 163.0 nM 6.79
CHEMBL202787 IC50 = 176.0 nM 6.75
CHEMBL203329 IC50 = 198.0 nM 6.70
CHEMBL206198 IC50 = 273.0 nM 6.56
CHEMBL205415 IC50 = 278.0 nM 6.56
CHEMBL383254 IC50 = 284.0 nM 6.55
CHEMBL205410 IC50 = 320.0 nM 6.50
CHEMBL205871 IC50 = 324.0 nM 6.49
CHEMBL381808 IC50 = 360.0 nM 6.44
CHEMBL204012 IC50 = 500.0 nM 6.30
CHEMBL383527 IC50 = 668.0 nM 6.17
CHEMBL203673 IC50 = 690.0 nM 6.16
CHEMBL202937 IC50 = 760.0 nM 6.12
CHEMBL203685 IC50 = 875.0 nM 6.06
CHEMBL202893 IC50 = 1100.0 nM 5.96
CHEMBL377294 IC50 = 2670.0 nM 5.57
CHEMBL381260 IC50 = 3110.0 nM 5.51
CHEMBL205514 IC50 = 3200.0 nM 5.50
CHEMBL206708 IC50 = 3340.0 nM 5.48
CHEMBL206236 IC50 = 4040.0 nM 5.39
CHEMBL206382 IC50 = 5080.0 nM 5.29
CHEMBL419932 IC50 = 5290.0 nM 5.28
CHEMBL203483 IC50 = 6350.0 nM 5.20
CHEMBL378823 IC50 = 6450.0 nM 5.19
CHEMBL203434 IC50 = 6760.0 nM 5.17
CHEMBL381829 IC50 = 8020.0 nM 5.10
CHEMBL204213 IC50 = 10870.0 nM 4.96
CHEMBL205820 IC50 = 14710.0 nM 4.83
CHEMBL204059 IC50 = 19320.0 nM 4.71
CHEMBL206654 IC50 = 23270.0 nM 4.63
CHEMBL380958 IC50 = 24010.0 nM 4.62
CHEMBL205645 IC50 = 23910.0 nM 4.62
CHEMBL206328 IC50 = 32250.0 nM 4.49
CHEMBL203004 IC50 = 43010.0 nM 4.37
CHEMBL205836 IC50 > 50000.0 nM -