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Assay Detail

CHEMBL861140

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Binding
Inhibition of DNA polymerase alpha
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA polymerase alpha catalytic subunit (CHEMBL1828)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthetic analogues of the manzamenones and plakoridines which inhibit DNA polymerase.
Doncaster JR, Etchells LL, Kershaw NM, Nakamura R, Ryan H, Takeuchi R, Sakaguchi K, Sardarian A, Whitehead RC.
Bioorg Med Chem Lett (2006) 16 : 2877 -2881
PubMed 16563761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.13 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380892 1 5.72
CHEMBL210047 1 5.72
CHEMBL449712 1 5.64
CHEMBL210096 1 5.48
CHEMBL380026 1 5.46
CHEMBL425779 E-ENEDIONE 1 5.43
CHEMBL366792 UNTENONE A 1 5.37
CHEMBL207651 1 5.16
CHEMBL381375 1 5.10
CHEMBL437883 1 5.05
CHEMBL208804 1 4.71
CHEMBL379409 1 4.70
CHEMBL437310 1 4.68
CHEMBL377599 1 4.60
CHEMBL210842 PLAKEVULIN A 1 4.18
CHEMBL207165 1 -
CHEMBL210764 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380892 IC50 = 1900.0 nM 5.72
CHEMBL210047 IC50 = 1900.0 nM 5.72
CHEMBL449712 IC50 = 2300.0 nM 5.64
CHEMBL210096 IC50 = 3300.0 nM 5.48
CHEMBL380026 IC50 = 3500.0 nM 5.46
CHEMBL425779 E-ENEDIONE IC50 = 3700.0 nM 5.43
CHEMBL366792 UNTENONE A IC50 = 4300.0 nM 5.37
CHEMBL207651 IC50 = 6900.0 nM 5.16
CHEMBL381375 IC50 = 7900.0 nM 5.10
CHEMBL437883 IC50 = 8900.0 nM 5.05
CHEMBL208804 IC50 = 19700.0 nM 4.71
CHEMBL379409 IC50 = 19900.0 nM 4.70
CHEMBL437310 IC50 = 21000.0 nM 4.68
CHEMBL377599 IC50 = 25000.0 nM 4.60
CHEMBL210842 PLAKEVULIN A IC50 = 66000.0 nM 4.18
CHEMBL207165 IC50 > 12500.0 nM -
CHEMBL210764 IC50 > 50000.0 nM -