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Assay Detail

CHEMBL5127750

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

Binding
Inhibition of PARP1 (unknown origin) incubated for 1 hr by chemiluminescence assay
8
Total Activities
8
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

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.
Cheng B, Pan W, Xing Y, Xiao Y, Chen J, Xu Z.
Eur J Med Chem (2022) 230 : 114109 -114109
PubMed 35051747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.63 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5176874 1 9.60
CHEMBL5188771 1 9.23
CHEMBL4461382 1 9.11
CHEMBL4438741 1 8.43
CHEMBL4470724 1 8.31
CHEMBL4744783 1 8.20
CHEMBL4758337 1 8.14
CHEMBL4541731 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176874 IC50 = 0.25 nM 9.60
CHEMBL5188771 IC50 = 0.59 nM 9.23
CHEMBL4461382 IC50 = 0.78 nM 9.11
CHEMBL4438741 IC50 = 3.75 nM 8.43
CHEMBL4470724 IC50 = 4.9 nM 8.31
CHEMBL4744783 IC50 = 6.3 nM 8.20
CHEMBL4758337 IC50 = 7.3 nM 8.14
CHEMBL4541731 IC50 = 9.6 nM 8.02