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Assay Detail

CHEMBL3395144

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

Binding
Inhibition of recombinant Plk1 (unknown origin) preincubated for 30 mins before recombinant Cdc25C substrate addition by ADP-Glo kinase assay
14
Total Activities
14
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

Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors.
Liu M, Huang J, Chen DX, Jiang C.
Bioorg Med Chem Lett (2015) 25 : 431 -434
PubMed 25556101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.93 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241855 RIGOSERTIB 3.0 1 8.05
CHEMBL3394764 1 6.89
CHEMBL3394763 1 6.39
CHEMBL3394766 1 6.02
CHEMBL3394757 1 5.74
CHEMBL3394765 1 5.73
CHEMBL3394758 1 5.72
CHEMBL3394759 1 5.68
CHEMBL1672002 THYMOQUINONE 2.0 1 5.66
CHEMBL3394762 1 5.58
CHEMBL3394768 1 5.54
CHEMBL3394761 1 5.46
CHEMBL3394760 1 5.32
CHEMBL3394767 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241855 RIGOSERTIB IC50 = 9.0 nM 8.05
CHEMBL3394764 IC50 = 130.0 nM 6.89
CHEMBL3394763 IC50 = 410.0 nM 6.39
CHEMBL3394766 IC50 = 960.0 nM 6.02
CHEMBL3394757 IC50 = 1820.0 nM 5.74
CHEMBL3394765 IC50 = 1880.0 nM 5.73
CHEMBL3394758 IC50 = 1910.0 nM 5.72
CHEMBL3394759 IC50 = 2100.0 nM 5.68
CHEMBL1672002 THYMOQUINONE IC50 = 2180.0 nM 5.66
CHEMBL3394762 IC50 = 2640.0 nM 5.58
CHEMBL3394768 IC50 = 2900.0 nM 5.54
CHEMBL3394761 IC50 = 3470.0 nM 5.46
CHEMBL3394760 IC50 = 4840.0 nM 5.32
CHEMBL3394767 IC50 = 5710.0 nM 5.24