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Assay Detail

CHEMBL947432

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

Binding
Inhibition of Akt2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

RAC-beta serine/threonine-protein kinase (CHEMBL2431)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.
Siu T, Li Y, Nagasawa J, Liang J, Tehrani L, Chua P, Jones RE, Defeo-Jones D, Barnett SF, Robinson RG.
Bioorg Med Chem Lett (2008) 18 : 4191 -4194
PubMed 18550373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.77 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443661 1 8.40
CHEMBL488428 1 8.10
CHEMBL446966 1 7.80
CHEMBL444136 1 7.68
CHEMBL446134 1 7.58
CHEMBL502393 1 7.48
CHEMBL447114 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443661 IC50 = 4.0 nM 8.40
CHEMBL488428 IC50 = 8.0 nM 8.10
CHEMBL446966 IC50 = 16.0 nM 7.80
CHEMBL444136 IC50 = 21.0 nM 7.68
CHEMBL446134 IC50 = 26.0 nM 7.58
CHEMBL502393 IC50 = 33.0 nM 7.48
CHEMBL447114 IC50 = 44.0 nM 7.36