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Assay Detail

CHEMBL5127793

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

Binding
Inhibition of PARP1 (unknown origin)
5
Total Activities
5
Compounds Tested
2
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 4 8.82 9.24
Ki 1 8.48 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137320 TALAZOPARIB 4.0 1 9.24
CHEMBL521686 OLAPARIB 4.0 1 8.85
CHEMBL1173055 RUCAPARIB 4.0 1 8.77
CHEMBL506871 VELIPARIB 3.0 1 8.48
CHEMBL1094636 NIRAPARIB 4.0 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137320 TALAZOPARIB IC50 = 0.57 nM 9.24
CHEMBL521686 OLAPARIB IC50 = 1.4 nM 8.85
CHEMBL1173055 RUCAPARIB IC50 = 1.7 nM 8.77
CHEMBL506871 VELIPARIB Ki = 3.3 nM 8.48
CHEMBL1094636 NIRAPARIB IC50 = 3.8 nM 8.42