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Assay Detail

CHEMBL812282

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

Binding
Compound was tested for topoisomerase II inhibition in purified HeLa cells by SDS/K+ precipitation method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

DNA topoisomerase II (CHEMBL2094255)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The antitumor activity of novel pyrazoloquinoline derivatives
Wentland MP, Aldous SC, Gruett MD, Perni RB, Powles RG, Danz DW, Klingbeil KM, Peverly A, Robinson RG, Corbett TH, Rake JB, Coughlin SA
Bioorg Med Chem Lett (1995) 5 : 405 -410
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.47 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132098 1 6.30
CHEMBL43 AMSACRINE 4.0 1 6.14
CHEMBL44657 ETOPOSIDE 4.0 1 6.09
CHEMBL130627 1 6.05
CHEMBL336549 1 5.77
CHEMBL131677 1 5.77
CHEMBL421899 1 5.77
CHEMBL130381 1 5.58
CHEMBL335683 1 5.57
CHEMBL131600 1 5.51
CHEMBL129908 1 5.50
CHEMBL133802 1 5.48
CHEMBL445908 1 5.38
CHEMBL131262 1 5.36
CHEMBL133466 1 5.23
CHEMBL133784 1 5.21
CHEMBL133757 1 5.19
CHEMBL130332 1 5.13
CHEMBL8179 WIN-57294 1 5.12
CHEMBL337180 1 5.01
CHEMBL334386 1 5.00
CHEMBL131491 1 4.96
CHEMBL414022 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132098 EC50 = 500.0 nM 6.30
CHEMBL43 AMSACRINE EC50 = 720.0 nM 6.14
CHEMBL44657 ETOPOSIDE EC50 = 810.0 nM 6.09
CHEMBL130627 EC50 = 900.0 nM 6.05
CHEMBL336549 EC50 = 1700.0 nM 5.77
CHEMBL131677 EC50 = 1700.0 nM 5.77
CHEMBL421899 EC50 = 1700.0 nM 5.77
CHEMBL130381 EC50 = 2600.0 nM 5.58
CHEMBL335683 EC50 = 2700.0 nM 5.57
CHEMBL131600 EC50 = 3100.0 nM 5.51
CHEMBL129908 EC50 = 3200.0 nM 5.50
CHEMBL133802 EC50 = 3300.0 nM 5.48
CHEMBL445908 EC50 = 4200.0 nM 5.38
CHEMBL131262 EC50 = 4400.0 nM 5.36
CHEMBL133466 EC50 = 5900.0 nM 5.23
CHEMBL133784 EC50 = 6100.0 nM 5.21
CHEMBL133757 EC50 = 6400.0 nM 5.19
CHEMBL130332 EC50 = 7400.0 nM 5.13
CHEMBL8179 WIN-57294 EC50 = 7600.0 nM 5.12
CHEMBL337180 EC50 = 9800.0 nM 5.01
CHEMBL334386 EC50 = 10000.0 nM 5.00
CHEMBL131491 EC50 = 11000.0 nM 4.96
CHEMBL414022 EC50 = 17000.0 nM 4.77