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Assay Detail

CHEMBL3364070

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

Binding
Inhibition of AKT1 (unknown origin) after 1 hr by Z'-LYTE kinase assay in presence of 75 uM ATP
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.
Nguyen T, Coover RA, Verghese J, Moran RG, Ellis KC.
ACS Med Chem Lett (2014) 5 : 462 -467
PubMed 24900862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494089 GSK-690693 1.0 1 9.22
CHEMBL1079175 MK-2206 2.0 1 8.00
CHEMBL3298512 1 6.24
CHEMBL3298516 1 5.35
CHEMBL3298929 1 5.33
CHEMBL3298792 1 4.79
CHEMBL3298611 1 4.61
CHEMBL3298513 1 -
CHEMBL3298514 1 -
CHEMBL3298515 1 -
CHEMBL3298610 1 -
CHEMBL3298928 1 -
CHEMBL3358446 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494089 GSK-690693 IC50 = 0.6 nM 9.22
CHEMBL1079175 MK-2206 IC50 = 10.0 nM 8.00
CHEMBL3298512 IC50 = 580.0 nM 6.24
CHEMBL3298516 IC50 = 4480.0 nM 5.35
CHEMBL3298929 IC50 = 4680.0 nM 5.33
CHEMBL3298792 IC50 = 16130.0 nM 4.79
CHEMBL3298611 IC50 = 24660.0 nM 4.61
CHEMBL3298513 IC50 > 100000.0 nM -
CHEMBL3298514 IC50 > 100000.0 nM -
CHEMBL3298515 IC50 > 100000.0 nM -
CHEMBL3298610 IC50 > 100000.0 nM -
CHEMBL3298928 IC50 > 100000.0 nM -
CHEMBL3358446 IC50 > 100000.0 nM -