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Assay Detail

CHEMBL5132147

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

Binding
Inhibition of human PARP2 using NAD+ as substrate incubated for 1 hr by ELISA
9
Total Activities
9
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

Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.
Yu J, Luo L, Hu T, Cui Y, Sun X, Gou W, Hou W, Li Y, Sun T.
Eur J Med Chem (2022) 227 : 113898 -113898
PubMed 34656898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.23 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173055 RUCAPARIB 4.0 1 9.30
CHEMBL5203682 1 8.54
CHEMBL5182785 1 8.38
CHEMBL5170407 1 8.24
CHEMBL5183006 1 8.19
CHEMBL5174694 1 8.18
CHEMBL5193574 1 8.10
CHEMBL5208255 1 7.95
CHEMBL5197357 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173055 RUCAPARIB IC50 = 0.5 nM 9.30
CHEMBL5203682 IC50 = 2.91 nM 8.54
CHEMBL5182785 IC50 = 4.21 nM 8.38
CHEMBL5170407 IC50 = 5.71 nM 8.24
CHEMBL5183006 IC50 = 6.4 nM 8.19
CHEMBL5174694 IC50 = 6.68 nM 8.18
CHEMBL5193574 IC50 = 8.04 nM 8.10
CHEMBL5208255 IC50 = 11.21 nM 7.95
CHEMBL5197357 IC50 = 61.9 nM 7.21