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Assay Detail

CHEMBL3424869

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

Binding
Inhibition of GST-tagged Tankyrases 1 (unknown origin) by autoPARsylationassay
2
Total Activities
2
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 tankyrase-1 (CHEMBL6164)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.
Nencini A, Pratelli C, Quinn JM, Salerno M, Tunici P, De Robertis A, Valensin S, Mennillo F, Rossi M, Bakker A, Benicchi T, Cappelli F, Turlizzi E, Nibbio M, Caradonna NP, Zanelli U, Andreini M, Magnani M, Varrone M.
Eur J Med Chem (2015) 95 : 526 -545
PubMed 25847770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.36 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431805 1 7.96
CHEMBL3422630 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431805 IC50 = 11.0 nM 7.96
CHEMBL3422630 IC50 = 18000.0 nM 4.75