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Assay Detail

CHEMBL5228293

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

Binding
Inhibition of N-terminal FLAG-tagged human recombinant PARP7 (400 to 657 residues) expressed in Sf9 insect cells by chemiluminescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein mono-ADP-ribosyltransferase TIPARP (CHEMBL2380188)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models.
Buchstaller HP, Anlauf U, Dorsch D, Kögler S, Kuhn D, Lehmann M, Leuthner B, Lodholz S, Musil D, Radtki D, Rettig C, Ritzert C, Rohdich F, Schneider R, Wegener A, Weigt S, Wilkinson K, Esdar C.
J Med Chem (2021) 64 : 10371 -10392
PubMed 34255518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.48 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199558 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199558 IC50 = 330.0 nM 6.48