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

CHEMBL663645

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

Binding
Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
Luzzio MJ, Besterman JM, Emerson DL, Evans MG, Lackey K, Leitner PL, McIntyre G, Morton B, Myers PL, Peel M.
J Med Chem (1995) 38 : 395 -401
PubMed 7853331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.85 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338843 1 7.96
CHEMBL335455 1 7.82
CHEMBL307794 1 7.11
CHEMBL128315 1 6.52
CHEMBL341028 1 6.38
CHEMBL65 CAMPTOTHECIN -1.0 1 6.17
CHEMBL84 TOPOTECAN 4.0 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338843 IC50 = 11.0 nM 7.96
CHEMBL335455 IC50 = 15.0 nM 7.82
CHEMBL307794 IC50 = 78.0 nM 7.11
CHEMBL128315 IC50 = 300.0 nM 6.52
CHEMBL341028 IC50 = 416.0 nM 6.38
CHEMBL65 CAMPTOTHECIN IC50 = 679.0 nM 6.17
CHEMBL84 TOPOTECAN IC50 = 1028.0 nM 5.99