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Assay Detail

CHEMBL5369702

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

Binding
Inhibition of N-terminal GST-tagged human PARP2 (2 to 583 residues) expressed in baculovirus-infected Sf9 cells using histone as substrate incubated for 60 mins in presence of activated DNA, NAD+, NAD+-biotin by luminescence based analysis
3
Total Activities
3
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

Poly [ADP-ribose] polymerase 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Expanding the Role of Boron in New Drug Chemotypes: Properties, Chemistry, Pharmaceutical Potential of Hemiboronic Naphthoids.
Kazmi MZH, Schneider OM, Hall DG.
J Med Chem (2023) 66 : 13768 -13787
PubMed 37752013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.41 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521686 OLAPARIB 4.0 1 9.89
CHEMBL5440473 1 6.92
CHEMBL5435592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521686 OLAPARIB IC50 = 0.13 nM 9.89
CHEMBL5440473 IC50 = 120.0 nM 6.92
CHEMBL5435592 IC50 > 1000.0 nM -