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Assay Detail

CHEMBL941578

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

Functional
Antiproliferative activity against human HCT116 cells after 3 days by methylene blue stain technique
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
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 36 5.53 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514499 GW843682X 1 6.16
CHEMBL474028 1 6.03
CHEMBL514162 GW852849X 1 6.00
CHEMBL475857 1 5.96
CHEMBL474053 1 5.94
CHEMBL474843 1 5.91
CHEMBL480545 1 5.83
CHEMBL480383 1 5.82
CHEMBL480382 GSK-312948A 1 5.81
CHEMBL519120 1 5.77
CHEMBL475763 1 5.75
CHEMBL474054 1 5.68
CHEMBL475783 1 5.64
CHEMBL514634 1 5.58
CHEMBL474029 1 5.58
CHEMBL514968 1 5.57
CHEMBL514826 1 5.53
CHEMBL520080 1 5.51
CHEMBL473630 1 5.47
CHEMBL475616 1 5.46
CHEMBL481510 GW853606X 1 5.45
CHEMBL475215 1 5.26
CHEMBL474432 1 5.12
CHEMBL516362 1 5.11
CHEMBL514643 1 4.92
CHEMBL519286 1 4.72
CHEMBL475762 1 4.68
CHEMBL473629 GSK-204925A 1 4.62
CHEMBL481492 1 -
CHEMBL519289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514499 GW843682X IC50 = 699.0 nM 6.16
CHEMBL474028 IC50 = 926.0 nM 6.03
CHEMBL514162 GW852849X IC50 = 999.0 nM 6.00
CHEMBL475857 IC50 = 1090.0 nM 5.96
CHEMBL474053 IC50 = 1150.0 nM 5.94
CHEMBL474843 IC50 = 1230.0 nM 5.91
CHEMBL480545 IC50 = 1480.0 nM 5.83
CHEMBL480383 IC50 = 1520.0 nM 5.82
CHEMBL480382 GSK-312948A IC50 = 1540.0 nM 5.81
CHEMBL519120 IC50 = 1690.0 nM 5.77
CHEMBL475763 IC50 = 1770.0 nM 5.75
CHEMBL474054 IC50 = 2110.0 nM 5.68
CHEMBL475783 IC50 = 2270.0 nM 5.64
CHEMBL514634 IC50 = 2640.0 nM 5.58
CHEMBL474029 IC50 = 2630.0 nM 5.58
CHEMBL514968 IC50 = 2700.0 nM 5.57
CHEMBL514826 IC50 = 2960.0 nM 5.53
CHEMBL520080 IC50 = 3090.0 nM 5.51
CHEMBL473630 IC50 = 3380.0 nM 5.47
CHEMBL475616 IC50 = 3470.0 nM 5.46
CHEMBL481510 GW853606X IC50 = 3590.0 nM 5.45
CHEMBL475215 IC50 = 5430.0 nM 5.26
CHEMBL474432 IC50 = 7660.0 nM 5.12
CHEMBL516362 IC50 = 7750.0 nM 5.11
CHEMBL514643 IC50 = 12100.0 nM 4.92
CHEMBL519286 IC50 = 19000.0 nM 4.72
CHEMBL475762 IC50 = 21000.0 nM 4.68
CHEMBL473629 GSK-204925A IC50 = 24100.0 nM 4.62
CHEMBL481492 IC50 > 28000.0 nM -
CHEMBL519289 IC50 > 30000.0 nM -
CHEMBL219899 IC50 > 30000.0 nM -
CHEMBL482349 IC50 > 25000.0 nM -
CHEMBL480371 GW853609X IC50 > 30000.0 nM -
CHEMBL482151 IC50 > 30000.0 nM -
CHEMBL520284 IC50 > 30000.0 nM -
CHEMBL514040 IC50 > 30000.0 nM -