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Assay Detail

CHEMBL3225200

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

Binding
Inhibition of mouse recombinant PARP2 assessed as radioactivity incorporated from [adenine-2,8-3H]NAD into proteins by liquid scintillation spectrometry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Poly [ADP-ribose] polymerase 2 (CHEMBL2794)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ
Pellicciari R, Camaioni E, Gilbert AM, Macchiarulo A, Bikker JA, Shah F, Bard J, Costantino G, Gioiello A, Robertson GM, Sabbatini P, Venturoni F, Liscio P, Carotti A, Bellocchi D, Cozzi A, Wood A, Gonzales C, Zaleska MM, Ellingboe JW, Moroni F
Medchemcomm (2011) 2 : 559 -565
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.72 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3219283 1 7.42
CHEMBL3219282 1 6.52
CHEMBL3108871 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3219283 IC50 = 38.0 nM 7.42
CHEMBL3219282 IC50 = 300.0 nM 6.52
CHEMBL3108871 IC50 = 600.0 nM 6.22