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Assay Detail

CHEMBL1046490

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

Binding
Inhibition of calf thymus DNA polymerase alpha by [3H]dTTP incorporation assay
16
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 16 6.64 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594272 2 7.22
CHEMBL595189 2 7.05
CHEMBL594951 2 6.75
CHEMBL594273 2 6.62
CHEMBL594151 DEHYDROALTENUSIN 2 6.17
CHEMBL611034 DESMETHYLDEHYDROALTENUSIN 2 6.05
CHEMBL593327 1 -
CHEMBL593328 1 -
CHEMBL595213 1 -
CHEMBL595214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594272 IC50 = 60.0 nM 7.22
CHEMBL595189 IC50 = 90.0 nM 7.05
CHEMBL594951 IC50 = 180.0 nM 6.75
CHEMBL594273 IC50 = 240.0 nM 6.62
CHEMBL594151 DEHYDROALTENUSIN IC50 = 680.0 nM 6.17
CHEMBL611034 DESMETHYLDEHYDROALTENUSIN IC50 = 890.0 nM 6.05
CHEMBL593327 IC50 > 200000.0 nM -
CHEMBL593328 IC50 > 200000.0 nM -
CHEMBL595213 IC50 > 200000.0 nM -
CHEMBL595214 IC50 > 200000.0 nM -
CHEMBL594151 DEHYDROALTENUSIN IC50 - -
CHEMBL611034 DESMETHYLDEHYDROALTENUSIN IC50 - -
CHEMBL594951 IC50 - -
CHEMBL595189 IC50 - -
CHEMBL594272 IC50 - -
CHEMBL594273 IC50 - -