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Assay Detail

CHEMBL937419

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Binding
Inhibition of Akt1 by cell-based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Bilodeau MT, Balitza AE, Hoffman JM, Manley PJ, Barnett SF, Defeo-Jones D, Haskell K, Jones RE, Leander K, Robinson RG, Smith AM, Huber HE, Hartman GD.
Bioorg Med Chem Lett (2008) 18 : 3178 -3182
PubMed 18479914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.07 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262341 1 7.80
CHEMBL259967 1 7.68
CHEMBL259753 1 7.52
CHEMBL259968 1 7.51
CHEMBL260670 1 7.08
CHEMBL260184 1 6.88
CHEMBL259982 1 6.83
CHEMBL258844 1 6.70
CHEMBL261540 1 6.43
CHEMBL258696 1 6.28
CHEMBL429703 1 -
CHEMBL407733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262341 IC50 = 16.0 nM 7.80
CHEMBL259967 IC50 = 21.0 nM 7.68
CHEMBL259753 IC50 = 30.0 nM 7.52
CHEMBL259968 IC50 = 31.0 nM 7.51
CHEMBL260670 IC50 = 83.0 nM 7.08
CHEMBL260184 IC50 = 132.0 nM 6.88
CHEMBL259982 IC50 = 149.0 nM 6.83
CHEMBL258844 IC50 = 200.0 nM 6.70
CHEMBL261540 IC50 = 369.0 nM 6.43
CHEMBL258696 IC50 = 527.0 nM 6.28
CHEMBL429703 IC50 - -
CHEMBL407733 IC50 - -