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Assay Detail

CHEMBL5366430

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

Binding
Inhibition of PARP4 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay
2
Total Activities
2
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 PARP4 (CHEMBL6142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

YCH1899, a Highly Effective Phthalazin-1(2<i>H</i>)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors.
Sun Y, Yang H, Yuan J, Wang L, Song S, Chen R, Bao X, Jia L, Yang T, Zhang X, He Q, Gan Y, Miao Z, He J, Yang C.
J Med Chem (2023) 66 : 12284 -12303
PubMed 37605459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.44 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5402698 1 9.00
CHEMBL521686 OLAPARIB 4.0 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5402698 IC50 = 1.0 nM 9.00
CHEMBL521686 OLAPARIB IC50 = 13.5 nM 7.87