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Assay Detail

CHEMBL658099

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

Binding
Compound was evaluated for the inhibition of cellular DNA polymerase (beta)
9
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA polymerase beta (CHEMBL2392)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'-deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta, and epsilon nor HIV-1 reverse transcriptase.
von Janta-Lipinski M, Costisella B, Ochs H, Hübscher U, Hafkemeyer P, Matthes E.
J Med Chem (1998) 41 : 2040 -2046
PubMed 9622545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.80 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483492 2 6.00
CHEMBL2092835 2 6.00
CHEMBL2092833 2 5.66
CHEMBL2092834 2 5.52
CHEMBL220940 THYMIDINE_TRIPHOSPHATE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483492 IC50 = 1000.0 nM 6.00
CHEMBL2092835 IC50 = 1000.0 nM 6.00
CHEMBL2092833 IC50 = 2200.0 nM 5.66
CHEMBL2092834 IC50 = 3000.0 nM 5.52
CHEMBL220940 THYMIDINE_TRIPHOSPHATE IC50 > 200000.0 nM -
CHEMBL2092835 IC50 > 100000.0 nM -
CHEMBL483492 IC50 > 200000.0 nM -
CHEMBL2092833 IC50 > 200000.0 nM -
CHEMBL2092834 IC50 > 100000.0 nM -