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Assay Detail

CHEMBL3807232

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

Binding
Inhibition of human recombinant His-tagged PARP1 autoparsylation expressed in sf21 cells using NAD and biotinylated NAD incubated for 150 mins by HTRF assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.
Abdel-Magid AF.
ACS Med Chem Lett (2016) 7 : 209 -210
PubMed 26985304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.09 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3805627 1 6.92
CHEMBL3805896 1 6.14
CHEMBL3805393 1 5.92
CHEMBL3806049 1 5.75
CHEMBL3804939 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3805627 IC50 = 120.0 nM 6.92
CHEMBL3805896 IC50 = 730.0 nM 6.14
CHEMBL3805393 IC50 = 1200.0 nM 5.92
CHEMBL3806049 IC50 = 1800.0 nM 5.75
CHEMBL3804939 IC50 = 1900.0 nM 5.72