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Assay Detail

CHEMBL4305080

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

Binding
Inhibition of human PARP2 expressed in Escherichia coli using biotinylated histone H1 as substrate measured in presence of [3H]NAD+ by topcount scintillation counting method
1
Total Activities
1
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 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity.
Velagapudi UK, Langelier MF, Delgado-Martin C, Diolaiti ME, Bakker S, Ashworth A, Patel BA, Shao X, Pascal JM, Talele TT.
J Med Chem (2019) 62 : 5330 -5357
PubMed 31042381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.54 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506871 VELIPARIB 3.0 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506871 VELIPARIB IC50 = 2.9 nM 8.54