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Assay Detail

CHEMBL5123573

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

Functional
Rescue of cell viability in human HeLa cells expressing wild type PARP10 at upto 10 uM incubated for 10 to 12 days by methylene blue dye based colony formation assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for mono-ADP-ribosyltransferases PARP10 and PARP15.
Nizi MG, Maksimainen MM, Murthy S, Massari S, Alaviuhkola J, Lippok BE, Sowa ST, Galera-Prat A, Prunskaite-Hyyryläinen R, Lüscher B, Korn P, Lehtiö L, Tabarrini O.
Eur J Med Chem (2022) 237 : 114362 -114362
PubMed 35500474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.97 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186967 1 6.23
CHEMBL5200521 1 6.02
CHEMBL5181947 1 5.82
CHEMBL5200358 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186967 EC50 = 590.0 nM 6.23
CHEMBL5200521 EC50 = 950.0 nM 6.02
CHEMBL5181947 EC50 = 1500.0 nM 5.82
CHEMBL5200358 EC50 = 1600.0 nM 5.80