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Assay Detail

CHEMBL4220028

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

Binding
Inhibition of PDK1 mediated PI3K/Akt/mTOR pathway activation in human AN3CA cells assessed as reduction in ribosomal p70S6 protein phosphorylation after 2 hrs by in-cell Western blotting analysis
2
Total Activities
2
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

3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors.
Chen T, Sorna V, Choi S, Call L, Bearss J, Carpenter K, Warner SL, Sharma S, Bearss DJ, Vankayalapati H.
Bioorg Med Chem Lett (2017) 27 : 5473 -5480
PubMed 29150397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.12 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3659990 1 7.12
CHEMBL3659991 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3659990 EC50 = 75.6 nM 7.12
CHEMBL3659991 EC50 = 76.7 nM 7.12