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Assay Detail

CHEMBL4707266

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

Binding
Inhibition of PI3K/AKT/mTOR signaling in human HepG2 cells assessed as reduction in EGF-stimulated phosphorylation of Akt at S473 residue incubated for 3 hrs followed by stimulation with 50 ng/ml growth factor EGF for 15 mins by by ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
Chen D,Soh CK,Goh WH,Wang H
J Med Chem (2018) 61 : 1552 -1575
PubMed 29360358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.63 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4744689 1 6.89
CHEMBL521851 PICTILISIB 2.0 1 6.77
CHEMBL4749655 1 6.24
CHEMBL98 VORINOSTAT 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4744689 EC50 = 130.0 nM 6.89
CHEMBL521851 PICTILISIB EC50 = 170.0 nM 6.77
CHEMBL4749655 EC50 = 580.0 nM 6.24
CHEMBL98 VORINOSTAT EC50 > 30000.0 nM -