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Assay Detail

CHEMBL5520515

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

Binding
Inhibition of human DNA polymerase theta (67 to 970 residues) ATPase activity expressed in Sf9 insect cells incubated for 40 mins by ADP-glo assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA polymerase theta (CHEMBL6025)
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 2 6.62 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566472 1 8.62
CHEMBL36506 NOVOBIOCIN 4.0 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566472 IC50 = 2.4 nM 8.62
CHEMBL36506 NOVOBIOCIN IC50 = 24000.0 nM 4.62