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Assay Detail

CHEMBL4259693

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Binding
Inhibition of AKT1 (unknown origin) using biotin-labelled STK as substrate measured after 45 mins by HTRF method
7
Total Activities
7
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

Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
Zhang D, Tong D, Yang D, Sun J, Zhang F, Zhao G.
Medchemcomm (2018) 9 : 1340 -1350
PubMed 30151089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.47 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494089 GSK-690693 1.0 1 7.67
CHEMBL4285143 1 7.61
CHEMBL4281435 1 7.57
CHEMBL4284849 1 7.52
CHEMBL4282775 1 7.48
CHEMBL4292059 1 7.29
CHEMBL4284420 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494089 GSK-690693 IC50 = 21.3 nM 7.67
CHEMBL4285143 IC50 = 24.3 nM 7.61
CHEMBL4281435 IC50 = 26.9 nM 7.57
CHEMBL4284849 IC50 = 30.5 nM 7.52
CHEMBL4282775 IC50 = 32.9 nM 7.48
CHEMBL4292059 IC50 = 51.9 nM 7.29
CHEMBL4284420 IC50 = 66.6 nM 7.18