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Assay Detail

CHEMBL911349

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Binding
Inhibition of PLK1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase.
Bamborough P, Christopher JA, Cutler GJ, Dickson MC, Mellor GW, Morey JV, Patel CB, Shewchuk LM.
Bioorg Med Chem Lett (2006) 16 : 6236 -6240
PubMed 16997559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.40 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219899 1 6.90
CHEMBL220032 1 6.60
CHEMBL219711 1 6.20
CHEMBL222312 1 6.20
CHEMBL373751 GSK-319347A 1 6.10
CHEMBL375787 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219899 IC50 = 125.89 nM 6.90
CHEMBL220032 IC50 = 251.19 nM 6.60
CHEMBL219711 IC50 = 630.96 nM 6.20
CHEMBL222312 IC50 = 630.96 nM 6.20
CHEMBL373751 GSK-319347A IC50 = 794.33 nM 6.10
CHEMBL375787 IC50 < 10000.0 nM -