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Assay Detail

CHEMBL3887958

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

Binding
Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.51 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3907010 1 9.66
CHEMBL521686 OLAPARIB 4.0 1 9.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3907010 IC50 = 0.22 nM 9.66
CHEMBL521686 OLAPARIB IC50 = 0.45 nM 9.35