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Assay Detail

CHEMBL4043455

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

Binding
Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate after 45 mins in presence of gamma-P33-ATP by radiometric kinase assay
1
Total Activities
1
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

Serine/threonine-protein kinase PLK1 (CHEMBL3024)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Liu Z, Wang P, Chen H, Wold EA, Tian B, Brasier AR, Zhou J.
J Med Chem (2017) 60 : 4533 -4558
PubMed 28195723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.08 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513909 BI-2536 2.0 1 9.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513909 BI-2536 IC50 = 0.83 nM 9.08