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Assay Detail

CHEMBL648233

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Functional
Inhibition of [14C]-cytidine incorporation into DNA in Burkitt''s lymphoma cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type lymphoma
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, cytotoxicity, and antitumor activity of copper(II) and iron(II) complexes of (4)N-azabicyclo[3.2.2]nonane thiosemicarbazones derived from acyl diazines.
Easmon J, Pürstinger G, Heinisch G, Roth T, Fiebig HH, Holzer W, Jäger W, Jenny M, Hofmann J.
J Med Chem (2001) 44 : 2164 -2171
PubMed 11405653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.86 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71931 N-[(1E)-1-(3-methylpyrazin-2-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex 1 6.75
CHEMBL307750 N-[(1E)-1-(6-methylpyrimidin-4-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex 1 6.68
CHEMBL68899 1 6.50
CHEMBL307351 1 5.68
CHEMBL303030 N-[(1E)-1-(5-methylpyrazin-2-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex 1 5.53
CHEMBL68043 1 5.48
CHEMBL467 HYDROXYUREA 4.0 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71931 N-[(1E)-1-(3-methylpyrazin-2-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex IC50 = 180.0 nM 6.75
CHEMBL307750 N-[(1E)-1-(6-methylpyrimidin-4-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex IC50 = 210.0 nM 6.68
CHEMBL68899 IC50 = 320.0 nM 6.50
CHEMBL307351 IC50 = 2100.0 nM 5.68
CHEMBL303030 N-[(1E)-1-(5-methylpyrazin-2-yl)ethylidene]-3-azabicyclo[3.2.2]nonane-3-carbohydrazonothioic acid.chloro Cu(II)complex IC50 = 2970.0 nM 5.53
CHEMBL68043 IC50 = 3320.0 nM 5.48
CHEMBL467 HYDROXYUREA IC50 = 37150.0 nM 4.43