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Assay Detail

CHEMBL4627148

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

Binding
Inhibition of human GST-tagged tankyrase 2 autophosphorylation
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-2 (CHEMBL6154)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 4-Heteroarylcarbonyl-N-(phenyl or heteroaryl) Piperidine-1-carboxamides as Tankyrase Inhibitors.
Sabnis RW.
ACS Med Chem Lett (2020) 11 : 1676 -1677
PubMed 32944134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.56 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634919 1 9.72
CHEMBL4632401 1 9.60
CHEMBL4640008 1 9.59
CHEMBL4643690 1 9.57
CHEMBL4639702 1 9.54
CHEMBL4645574 1 9.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634919 IC50 = 0.19 nM 9.72
CHEMBL4632401 IC50 = 0.25 nM 9.60
CHEMBL4640008 IC50 = 0.26 nM 9.59
CHEMBL4643690 IC50 = 0.27 nM 9.57
CHEMBL4639702 IC50 = 0.29 nM 9.54
CHEMBL4645574 IC50 = 0.44 nM 9.36