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Assay Detail

CHEMBL3225202

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

Binding
Inhibition of human PARP1 in HEK293 cells assessed as prevention of in MNNG-induced ATP depletion
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

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
EC50 2 6.94 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3219283 1 7.85
CHEMBL45245 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3219283 EC50 = 14.0 nM 7.85
CHEMBL45245 EC50 = 945.0 nM 6.03