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Assay Detail

CHEMBL4121776

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

Binding
Inhibition of human PKA measured at apparent ATP Km level
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.64 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4129379 1 7.08
CHEMBL4129817 1 6.91
CHEMBL4126067 1 6.38
CHEMBL4128457 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4129379 IC50 = 84.0 nM 7.08
CHEMBL4129817 IC50 = 124.0 nM 6.91
CHEMBL4126067 IC50 = 412.0 nM 6.38
CHEMBL4128457 IC50 = 653.0 nM 6.18