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Assay Detail

CHEMBL3100280

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

Binding
Inhibition of recombinant AKT1 (unknown origin) using serine/threonine 06 peptide as substrate after 1 hr by FRET based Z'-LYTE assay
8
Total Activities
8
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

Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.
Korwar S, Nguyen T, Ellis KC.
Bioorg Med Chem Lett (2014) 24 : 271 -274
PubMed 24321345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.80 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.96
CHEMBL475400 1 7.36
CHEMBL522996 1 6.55
CHEMBL3099612 1 5.53
CHEMBL55934 NAPHTHOQUINONE 1 4.96
CHEMBL3099615 1 4.91
CHEMBL3099614 1 4.86
CHEMBL3099613 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 11.0 nM 7.96
CHEMBL475400 IC50 = 44.0 nM 7.36
CHEMBL522996 IC50 = 280.0 nM 6.55
CHEMBL3099612 IC50 = 2940.0 nM 5.53
CHEMBL55934 NAPHTHOQUINONE IC50 = 10980.0 nM 4.96
CHEMBL3099615 IC50 = 12270.0 nM 4.91
CHEMBL3099614 IC50 = 13670.0 nM 4.86
CHEMBL3099613 IC50 = 50000.0 nM 4.30