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Assay Detail

CHEMBL3807233

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

Binding
Inhibition of GST-tagged TNKS1 (1023 to 1327 residues) (unknown origin) autoparsylation using biotinylated NAD incubated for 1 hr by ELISA
6
Total Activities
6
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

Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.
Abdel-Magid AF.
ACS Med Chem Lett (2016) 7 : 209 -210
PubMed 26985304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.27 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3805896 1 9.74
CHEMBL3806163 1 9.70
CHEMBL3805393 1 9.62
CHEMBL3804939 1 9.40
CHEMBL3806049 1 9.09
CHEMBL3805627 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3805896 IC50 = 0.18 nM 9.74
CHEMBL3806163 IC50 = 0.2 nM 9.70
CHEMBL3805393 IC50 = 0.24 nM 9.62
CHEMBL3804939 IC50 = 0.4 nM 9.40
CHEMBL3806049 IC50 = 0.81 nM 9.09
CHEMBL3805627 IC50 = 8.5 nM 8.07