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Assay Detail

CHEMBL2330714

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

Binding
Inhibition of PARP1/PARP2 in human SKOV3 cells assessed as reduction in H2O2-induced PARylation incubated for 4 hrs prior to H2O2 treatment
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-OV-3
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

PARP 1, 2 and 3 (CHEMBL3390820)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.
Ye N, Chen CH, Chen T, Song Z, He JX, Huan XJ, Song SS, Liu Q, Chen Y, Ding J, Xu Y, Miao ZH, Zhang A.
J Med Chem (2013) 56 : 2885 -2903
PubMed 23473053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.06 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2323226 1 9.31
CHEMBL521686 OLAPARIB 4.0 1 7.68
CHEMBL2322618 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2323226 IC50 = 0.49 nM 9.31
CHEMBL521686 OLAPARIB IC50 = 20.9 nM 7.68
CHEMBL2322618 IC50 = 66.1 nM 7.18