Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL813222

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

Binding
Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HL-60
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
Wall ME, Wani MC, Nicholas AW, Manikumar G, Tele C, Moore L, Truesdale A, Leitner P, Besterman JM.
J Med Chem (1993) 36 : 2689 -2700
PubMed 8410981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.21 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52057 1 7.42
CHEMBL90761 1 7.16
CHEMBL315269 RS-9-Aminocamptothecin 1 6.08
CHEMBL276820 1 5.80
CHEMBL545250 1 5.60
CHEMBL539032 1 5.17
CHEMBL558618 1 -
CHEMBL540569 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52057 IC50 = 38.0 nM 7.42
CHEMBL90761 IC50 = 69.0 nM 7.16
CHEMBL315269 RS-9-Aminocamptothecin IC50 = 840.0 nM 6.08
CHEMBL276820 IC50 = 1600.0 nM 5.80
CHEMBL545250 IC50 = 2500.0 nM 5.60
CHEMBL539032 IC50 = 6800.0 nM 5.17
CHEMBL558618 IC50 > 30000.0 nM -
CHEMBL540569 IC50 > 30000.0 nM -