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Assay Detail

CHEMBL4003520

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Binding
Inhibition of PARP4 (unknown origin)
9
Total Activities
7
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

Protein mono-ADP-ribosyltransferase PARP4 (CHEMBL6142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
Nathubhai A, Haikarainen T, Koivunen J, Murthy S, Koumanov F, Lloyd MD, Holman GD, Pihlajaniemi T, Tosh D, Lehtiö L, Threadgill MD.
J Med Chem (2017) 60 : 814 -820
PubMed 27983846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.18 4.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069447 2 4.19
CHEMBL4098188 2 4.16
CHEMBL4080163 1 -
CHEMBL1892587 1 -
CHEMBL4063631 1 -
CHEMBL1956162 1 -
CHEMBL4059827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069447 IC50 = 64565.42 nM 4.19
CHEMBL4069447 IC50 = 65000.0 nM 4.19
CHEMBL4098188 IC50 = 69183.1 nM 4.16
CHEMBL4098188 IC50 = 69000.0 nM 4.16
CHEMBL4080163 IC50 - -
CHEMBL1892587 IC50 - -
CHEMBL4063631 IC50 - -
CHEMBL1956162 IC50 - -
CHEMBL4059827 IC50 - -