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Assay Detail

CHEMBL814847

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

Binding
Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay
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 (CHEMBL2814)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
Kim DK, Ryu DH, Lee JY, Lee N, Kim YW, Kim JS, Chang K, Im GJ, Kim TK, Choi WS.
J Med Chem (2001) 44 : 1594 -1602
PubMed 11334569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.82 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN 2.0 1 5.40
CHEMBL289665 1 5.30
CHEMBL445883 1 4.92
CHEMBL296862 1 4.80
CHEMBL84 TOPOTECAN 4.0 1 4.70
CHEMBL297811 1 4.68
CHEMBL65 CAMPTOTHECIN -1.0 1 4.40
CHEMBL44044 1 4.39
CHEMBL288053 1 -
CHEMBL41652 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN IC50 = 4000.0 nM 5.40
CHEMBL289665 IC50 = 5000.0 nM 5.30
CHEMBL445883 IC50 = 12000.0 nM 4.92
CHEMBL296862 IC50 = 16000.0 nM 4.80
CHEMBL84 TOPOTECAN IC50 = 20000.0 nM 4.70
CHEMBL297811 IC50 = 21000.0 nM 4.68
CHEMBL65 CAMPTOTHECIN IC50 = 40000.0 nM 4.40
CHEMBL44044 IC50 = 41000.0 nM 4.39
CHEMBL288053 IC50 = 1600000.0 nM -
CHEMBL41652 IC50 = 133000.0 nM -