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Assay Detail

CHEMBL3826032

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

Binding
Inhibition of PDK1 (unknown origin) by FRET-based Z-lyte assay
5
Total Activities
5
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

Locking PDK1 in DFG-out conformation through 2-oxo-indole containing molecules: Another tools to fight glioblastoma.
Sestito S, Daniele S, Nesi G, Zappelli E, Di Maio D, Marinelli L, Digiacomo M, Lapucci A, Martini C, Novellino E, Rapposelli S.
Eur J Med Chem (2016) 118 : 47 -63
PubMed 27123901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.12 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824119 1 6.95
CHEMBL3823844 1 6.38
CHEMBL3824264 1 6.29
CHEMBL3823622 1 5.82
CHEMBL3822974 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3824119 IC50 = 112.0 nM 6.95
CHEMBL3823844 IC50 = 416.0 nM 6.38
CHEMBL3824264 IC50 = 512.0 nM 6.29
CHEMBL3823622 IC50 = 1520.0 nM 5.82
CHEMBL3822974 IC50 = 6680.0 nM 5.17