Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5217245

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

Binding
Inhibition of AKT2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 120 mins by hotspot kinase assay
4
Total Activities
4
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-beta serine/threonine-protein kinase (CHEMBL2431)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.
Yu X, Xu J, Cahuzac KM, Xie L, Shen Y, Chen X, Liu J, Parsons RE, Jin J.
J Med Chem (2022) 65 : 14237 -14260
PubMed 36197750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.31 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297188 MIRANSERTIB 2.0 1 8.85
CHEMBL5220876 1 7.07
CHEMBL5221128 1 7.05
CHEMBL5220918 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297188 MIRANSERTIB IC50 = 1.4 nM 8.85
CHEMBL5220876 IC50 = 86.0 nM 7.07
CHEMBL5221128 IC50 = 90.0 nM 7.05
CHEMBL5220918 IC50 = 558.0 nM 6.25