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Assay Detail

CHEMBL4121773

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

Binding
Inhibition of human recombinant AKT1 expressed in insect cells incubated for 60 mins measured at apparent ATP Km level by kinase ADP-FP 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-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Parthasarathy S, Henry K, Pei H, Clayton J, Rempala M, Johns D, De Frutos O, Garcia P, Mateos C, Pleite S, Wang Y, Stout S, Condon B, Ashok S, Lu Z, Ehlhardt W, Raub T, Lai M, Geeganage S, Burkholder TP.
Bioorg Med Chem Lett (2018) 28 : 1887 -1891
PubMed 29655979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.30 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128457 1 8.52
CHEMBL4126067 1 8.40
CHEMBL4129379 1 8.30
CHEMBL4129817 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128457 IC50 = 3.0 nM 8.52
CHEMBL4126067 IC50 = 4.0 nM 8.40
CHEMBL4129379 IC50 = 5.0 nM 8.30
CHEMBL4129817 IC50 = 11.0 nM 7.96