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Assay Detail

CHEMBL821423

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

Binding
Concentration required to inhibit 50% relaxation of 250 ng of SV40 DNA obtained with 0.5 I.U topoisomerase I at 37 degrees C for 30 min
10
Total Activities
10
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 cytotoxic activity of alkylidene- and alkyl-substituted camptothecins
Candiani I, Bedeschi A, Cabri W, Zarini F, Visentin G, Capolongo L, Geroni C, Ciomei M
Bioorg Med Chem Lett (1997) 7 : 847 -850
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.09 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274070 9-AMINOCAMPTOTHECIN 2.0 1 5.75
CHEMBL413917 1 5.50
CHEMBL352800 1 5.38
CHEMBL355285 1 5.17
CHEMBL168822 1 4.95
CHEMBL168975 1 4.50
CHEMBL353588 1 4.38
CHEMBL354671 1 -
CHEMBL168505 1 -
CHEMBL352709 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274070 9-AMINOCAMPTOTHECIN IC50 = 1800.0 nM 5.75
CHEMBL413917 IC50 = 3200.0 nM 5.50
CHEMBL352800 IC50 = 4200.0 nM 5.38
CHEMBL355285 IC50 = 6700.0 nM 5.17
CHEMBL168822 IC50 = 11300.0 nM 4.95
CHEMBL168975 IC50 = 31900.0 nM 4.50
CHEMBL353588 IC50 = 41800.0 nM 4.38
CHEMBL354671 IC50 > 100000.0 nM -
CHEMBL168505 IC50 > 100000.0 nM -
CHEMBL352709 IC50 > 100000.0 nM -