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Assay Detail

CHEMBL941563

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

Binding
Inhibition of PLK1 expressed in baculovirus-infected Trichoplusia-ni cells by scintillation proximity assay
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Trichoplusia-ni
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of thiophene inhibitors of polo-like kinase.
Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA, Nailor KE, Salovich JM, Spehar GM, Cheung M.
Bioorg Med Chem Lett (2009) 19 : 1018 -1021
PubMed 19097784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 7.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474028 1 8.70
CHEMBL514499 GW843682X 1 8.70
CHEMBL474843 1 8.70
CHEMBL474432 1 8.70
CHEMBL480545 1 8.70
CHEMBL514162 GW852849X 1 8.70
CHEMBL519120 1 8.40
CHEMBL474053 1 8.30
CHEMBL482151 1 8.22
CHEMBL474029 1 8.22
CHEMBL474054 1 8.10
CHEMBL514968 1 8.10
CHEMBL481510 GW853606X 1 8.05
CHEMBL518953 GSK-1023156A 1 7.96
CHEMBL480382 GSK-312948A 1 7.96
CHEMBL474603 1 7.92
CHEMBL514826 1 7.92
CHEMBL475597 1 7.92
CHEMBL475857 1 7.92
CHEMBL449608 1 7.92
CHEMBL518956 1 7.92
CHEMBL514643 1 7.89
CHEMBL475763 1 7.85
CHEMBL508763 1 7.85
CHEMBL481491 1 7.82
CHEMBL514634 1 7.77
CHEMBL520080 1 7.77
CHEMBL480383 1 7.77
CHEMBL475783 1 7.68
CHEMBL481492 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474028 IC50 = 2.0 nM 8.70
CHEMBL514499 GW843682X IC50 = 2.0 nM 8.70
CHEMBL474843 IC50 = 2.0 nM 8.70
CHEMBL474432 IC50 = 2.0 nM 8.70
CHEMBL480545 IC50 = 2.0 nM 8.70
CHEMBL514162 GW852849X IC50 = 2.0 nM 8.70
CHEMBL519120 IC50 = 4.0 nM 8.40
CHEMBL474053 IC50 = 5.0 nM 8.30
CHEMBL474029 IC50 = 6.0 nM 8.22
CHEMBL482151 IC50 = 6.0 nM 8.22
CHEMBL474054 IC50 = 8.0 nM 8.10
CHEMBL514968 IC50 = 8.0 nM 8.10
CHEMBL481510 GW853606X IC50 = 9.0 nM 8.05
CHEMBL518953 GSK-1023156A IC50 = 11.0 nM 7.96
CHEMBL480382 GSK-312948A IC50 = 11.0 nM 7.96
CHEMBL474603 IC50 = 12.0 nM 7.92
CHEMBL518956 IC50 = 12.0 nM 7.92
CHEMBL449608 IC50 = 12.0 nM 7.92
CHEMBL475857 IC50 = 12.0 nM 7.92
CHEMBL475597 IC50 = 12.0 nM 7.92
CHEMBL514826 IC50 = 12.0 nM 7.92
CHEMBL514643 IC50 = 13.0 nM 7.89
CHEMBL475763 IC50 = 14.0 nM 7.85
CHEMBL508763 IC50 = 14.0 nM 7.85
CHEMBL481491 IC50 = 15.0 nM 7.82
CHEMBL514634 IC50 = 17.0 nM 7.77
CHEMBL480383 IC50 = 17.0 nM 7.77
CHEMBL520080 IC50 = 17.0 nM 7.77
CHEMBL475783 IC50 = 21.0 nM 7.68
CHEMBL481492 IC50 = 21.0 nM 7.68
CHEMBL445277 IC50 = 22.0 nM 7.66
CHEMBL482349 IC50 = 27.0 nM 7.57
CHEMBL516248 GW804482X IC50 = 28.0 nM 7.55
CHEMBL475215 IC50 = 31.0 nM 7.51
CHEMBL475616 IC50 = 31.0 nM 7.51
CHEMBL473630 IC50 = 34.0 nM 7.47
CHEMBL474437 IC50 = 35.0 nM 7.46
CHEMBL481724 IC50 = 61.0 nM 7.21
CHEMBL516362 IC50 = 61.0 nM 7.21
CHEMBL454196 IC50 = 70.0 nM 7.16
CHEMBL520284 IC50 = 73.0 nM 7.14
CHEMBL219899 IC50 = 75.0 nM 7.12
CHEMBL471789 GSK-1030059A IC50 = 85.0 nM 7.07
CHEMBL481156 IC50 = 100.0 nM 7.00
CHEMBL514040 IC50 = 99.0 nM 7.00
CHEMBL473629 GSK-204925A IC50 = 130.0 nM 6.89
CHEMBL475762 IC50 = 130.0 nM 6.89
CHEMBL519286 IC50 = 190.0 nM 6.72
CHEMBL519289 IC50 = 250.0 nM 6.60
CHEMBL480371 GW853609X IC50 = 300.0 nM 6.52