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Assay Detail

CHEMBL5217248

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

Binding
Induction of AKT degradation in MS21-resistant human SW620 cells harboring KRAS/BRAF mutant assessed as reduction in total AKT level incubated for 24 hrs by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SW620
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
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
EC50 1 7.64 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5221128 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5221128 EC50 = 23.0 nM 7.64