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Assay Detail

CHEMBL1046492

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Binding
Inhibition of rat DNA polymerase beta by [3H]dTTP incorporation assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA polymerase beta (CHEMBL4343)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors.
Kuramochi K, Fukudome K, Kuriyama I, Takeuchi T, Sato Y, Kamisuki S, Tsubaki K, Sugawara F, Yoshida H, Mizushina Y.
Bioorg Med Chem (2009) 17 : 7227 -7238
PubMed 19767211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.46 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594272 1 4.96
CHEMBL595189 1 4.62
CHEMBL594951 1 4.46
CHEMBL594151 DEHYDROALTENUSIN 1 4.19
CHEMBL594273 1 4.05
CHEMBL611034 DESMETHYLDEHYDROALTENUSIN 1 -
CHEMBL593327 1 -
CHEMBL593328 1 -
CHEMBL595213 1 -
CHEMBL595214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594272 IC50 = 11000.0 nM 4.96
CHEMBL595189 IC50 = 24000.0 nM 4.62
CHEMBL594951 IC50 = 35000.0 nM 4.46
CHEMBL594151 DEHYDROALTENUSIN IC50 = 64000.0 nM 4.19
CHEMBL594273 IC50 = 89000.0 nM 4.05
CHEMBL611034 DESMETHYLDEHYDROALTENUSIN IC50 = 126000.0 nM -
CHEMBL593327 IC50 > 200000.0 nM -
CHEMBL593328 IC50 > 200000.0 nM -
CHEMBL595213 IC50 > 200000.0 nM -
CHEMBL595214 IC50 > 200000.0 nM -