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Assay Detail

CHEMBL5520552

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

Binding
Inhibition of human PARP1 incubated for 90 mins by colorimetric assay
7
Total Activities
7
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

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

Publication

Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
Ma L, Chen W, Yang M, Ha S, Xiong S, Zhu J, Xiang H, Luo G.
J Med Chem (2024) 67 : 3606 -3625
PubMed 38375763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.67 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521686 OLAPARIB 4.0 1 9.40
CHEMBL5556723 1 8.33
CHEMBL5558410 1 8.27
CHEMBL5564238 1 -
CHEMBL5555891 1 -
CHEMBL5566472 1 -
CHEMBL36506 NOVOBIOCIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521686 OLAPARIB IC50 = 0.4 nM 9.40
CHEMBL5556723 IC50 = 4.7 nM 8.33
CHEMBL5558410 IC50 = 5.4 nM 8.27
CHEMBL5564238 IC50 - -
CHEMBL5555891 IC50 - -
CHEMBL5566472 IC50 - -
CHEMBL36506 NOVOBIOCIN IC50 - -