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Assay Detail

CHEMBL5373880

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

Binding
Inhibition of PARP7 (unknown origin)
3
Total Activities
3
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

Protein mono-ADP-ribosyltransferase TIPARP (CHEMBL2380188)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Quinazoline-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, <i>In Vivo</i> Antitumor Activity, and X-ray Crystal Structure Analysis.
Zhou J, Du T, Wang X, Yao H, Deng J, Li Y, Chen X, Sheng L, Ji M, Xu B.
J Med Chem (2023) 66 : 14095 -14115
PubMed 37843892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.83 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5095043 ATAMPARIB 1.0 1 8.52
CHEMBL5402698 1 8.14
CHEMBL5420649 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5095043 ATAMPARIB IC50 = 3.0 nM 8.52
CHEMBL5402698 IC50 = 7.3 nM 8.14
CHEMBL5420649 IC50 = 149.0 nM 6.83