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Assay Detail

CHEMBL2433123

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

Binding
Inhibition of human full length ARTD2 using NAD+ as substrate by fluorescence assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Poly [ADP-ribose] polymerase 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.
Narwal M, Koivunen J, Haikarainen T, Obaji E, Legala OE, Venkannagari H, Joensuu P, Pihlajaniemi T, Lehtiö L.
J Med Chem (2013) 56 : 7880 -7889
PubMed 24116873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.11 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431805 2 6.32
CHEMBL64780 2 5.08
CHEMBL16861 2 4.56
CHEMBL2431867 2 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431805 IC50 = 478.63 nM 6.32
CHEMBL2431805 IC50 = 479.0 nM 6.32
CHEMBL64780 IC50 = 8317.64 nM 5.08
CHEMBL64780 IC50 = 8300.0 nM 5.08
CHEMBL16861 IC50 = 27542.29 nM 4.56
CHEMBL16861 IC50 = 27800.0 nM 4.56
CHEMBL2431867 IC50 = 34673.69 nM 4.46
CHEMBL2431867 IC50 = 34900.0 nM 4.46