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Assay Detail

CHEMBL4200425

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Binding
Inhibition of human recombinant PLK1 by Z-Lyte assay
25
Total Activities
25
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

Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.
Liu S, Yosief HO, Dai L, Huang H, Dhawan G, Zhang X, Muthengi AM, Roberts J, Buckley DL, Perry JA, Wu L, Bradner JE, Qi J, Zhang W.
J Med Chem (2018) 61 : 7785 -7795
PubMed 30125504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.48 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209902 1 8.96
CHEMBL4207165 1 8.40
CHEMBL4215729 1 8.40
CHEMBL513909 BI-2536 2.0 1 8.40
CHEMBL4216442 1 8.08
CHEMBL4202820 1 8.07
CHEMBL4216875 1 8.06
CHEMBL4213276 1 8.05
CHEMBL4206171 1 8.00
CHEMBL4210571 1 7.68
CHEMBL4206052 1 7.60
CHEMBL4203571 1 7.57
CHEMBL3609305 1 7.49
CHEMBL4214823 1 7.43
CHEMBL4207437 1 7.40
CHEMBL4209192 1 7.33
CHEMBL3609304 1 7.27
CHEMBL4215910 1 7.11
CHEMBL4202678 1 7.02
CHEMBL4206381 1 6.90
CHEMBL4210414 1 6.80
CHEMBL4212237 1 6.66
CHEMBL4207347 1 6.49
CHEMBL4212346 1 6.34
CHEMBL4218106 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209902 IC50 = 1.1 nM 8.96
CHEMBL4207165 IC50 = 4.0 nM 8.40
CHEMBL4215729 IC50 = 4.0 nM 8.40
CHEMBL513909 BI-2536 IC50 = 4.0 nM 8.40
CHEMBL4216442 IC50 = 8.4 nM 8.08
CHEMBL4202820 IC50 = 8.6 nM 8.07
CHEMBL4216875 IC50 = 8.7 nM 8.06
CHEMBL4213276 IC50 = 9.0 nM 8.05
CHEMBL4206171 IC50 = 9.9 nM 8.00
CHEMBL4210571 IC50 = 21.0 nM 7.68
CHEMBL4206052 IC50 = 25.2 nM 7.60
CHEMBL4203571 IC50 = 27.0 nM 7.57
CHEMBL3609305 IC50 = 32.5 nM 7.49
CHEMBL4214823 IC50 = 37.2 nM 7.43
CHEMBL4207437 IC50 = 40.0 nM 7.40
CHEMBL4209192 IC50 = 47.0 nM 7.33
CHEMBL3609304 IC50 = 54.1 nM 7.27
CHEMBL4215910 IC50 = 78.0 nM 7.11
CHEMBL4202678 IC50 = 95.0 nM 7.02
CHEMBL4206381 IC50 = 127.0 nM 6.90
CHEMBL4210414 IC50 = 160.0 nM 6.80
CHEMBL4212237 IC50 = 218.0 nM 6.66
CHEMBL4207347 IC50 = 322.0 nM 6.49
CHEMBL4212346 IC50 = 457.0 nM 6.34
CHEMBL4218106 IC50 = 2620.0 nM 5.58