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Assay Detail

CHEMBL663903

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

Binding
Inhibitory activity against DNA topoisomerase-1 obtained from Hela cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

DNA topoisomerase 1 (CHEMBL1781)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acylshikonin analogues: synthesis and inhibition of DNA topoisomerase-I.
Ahn BZ, Baik KU, Kweon GR, Lim K, Hwang BD.
J Med Chem (1995) 38 : 1044 -1047
PubMed 7699697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.23 4.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276448 1 4.40
CHEMBL8951 1 4.36
CHEMBL403516 ACETYLSHIKONIN 1 4.35
CHEMBL267024 DIMETHYLACRYLSHIKONIN 1 4.11
CHEMBL267275 1 4.10
CHEMBL9416 ISOBUTYLSHIKONIN 1 4.08
CHEMBL8937 1 -
CHEMBL9148 1 -
CHEMBL8806 1 -
CHEMBL9196 1 -
CHEMBL267435 1 -
CHEMBL9470 SHIKONIN 1 -
CHEMBL9499 1 -
CHEMBL65 CAMPTOTHECIN -1.0 1 -
CHEMBL269519 1 -
CHEMBL275029 1 -
CHEMBL9469 1 -
CHEMBL265619 1 -
CHEMBL9259 1 -
CHEMBL8805 1 -
CHEMBL9320 1 -
CHEMBL266603 1 -
CHEMBL8834 1 -
CHEMBL9523 1 -
CHEMBL9518 1 -
CHEMBL8794 1 -
CHEMBL9023 1 -
CHEMBL9266 1 -
CHEMBL9164 1 -
CHEMBL9338 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276448 IC50 = 40000.0 nM 4.40
CHEMBL8951 IC50 = 44000.0 nM 4.36
CHEMBL403516 ACETYLSHIKONIN IC50 = 45000.0 nM 4.35
CHEMBL267024 DIMETHYLACRYLSHIKONIN IC50 = 77000.0 nM 4.11
CHEMBL267275 IC50 = 80000.0 nM 4.10
CHEMBL9416 ISOBUTYLSHIKONIN IC50 = 84000.0 nM 4.08
CHEMBL9196 IC50 = 126000.0 nM -
CHEMBL8940 IC50 > 625000.0 nM -
CHEMBL267435 IC50 > 625000.0 nM -
CHEMBL9470 SHIKONIN IC50 = 208000.0 nM -
CHEMBL9499 IC50 = 161000.0 nM -
CHEMBL65 CAMPTOTHECIN IC50 = 127000.0 nM -
CHEMBL269519 IC50 > 625000.0 nM -
CHEMBL275029 IC50 > 625000.0 nM -
CHEMBL9469 IC50 > 625000.0 nM -
CHEMBL265619 IC50 = 207000.0 nM -
CHEMBL9148 IC50 = 130000.0 nM -
CHEMBL267049 IC50 > 625000.0 nM -
CHEMBL8804 IC50 = 222000.0 nM -
CHEMBL266355 IC50 > 625000.0 nM -
CHEMBL8806 IC50 = 144000.0 nM -
CHEMBL8937 IC50 > 625000.0 nM -
CHEMBL9259 IC50 > 625000.0 nM -
CHEMBL8805 IC50 = 153000.0 nM -
CHEMBL9320 IC50 = 250000.0 nM -
CHEMBL266603 IC50 = 153000.0 nM -
CHEMBL8834 IC50 = 137000.0 nM -
CHEMBL9523 IC50 > 625000.0 nM -
CHEMBL9518 IC50 > 625000.0 nM -
CHEMBL8794 IC50 = 115000.0 nM -
CHEMBL9023 IC50 > 625000.0 nM -
CHEMBL9266 IC50 = 153000.0 nM -
CHEMBL9164 IC50 = 625000.0 nM -
CHEMBL9338 IC50 > 625000.0 nM -