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Assay Detail

CHEMBL4340728

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

Binding
Inhibition of recombinant human N-terminal His6-fused PDK1 (M1 to M460 residues) expressed in Sf9 insect cells using tetra(LRRWSLG) peptide as substrate measured after 60 mins in presence of [gamma-33P]-ATP by scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.
Ostacolo C, Di Sarno V, Lauro G, Pepe G, Musella S, Ciaglia T, Vestuto V, Autore G, Bifulco G, Marzocco S, Campiglia P, Gomez-Monterrey IM, Bertamino A.
Eur J Med Chem (2019) 167 : 61 -75
PubMed 30763817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.96 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446681 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446681 IC50 = 11000.0 nM 4.96