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Assay Detail

CHEMBL4272745

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

Binding
Inhibition of N-terminal His-tagged human ARTD4 (250 to 565 residues) expressed in Escherichia coli Rosetta2 (DE3) using TCEP as substrate after 2.5 hrs in presence of NAD+
5
Total Activities
5
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

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.
Murthy S, Desantis J, Verheugd P, Maksimainen MM, Venkannagari H, Massari S, Ashok Y, Obaji E, Nkizinkinko Y, Lüscher B, Tabarrini O, Lehtiö L.
Eur J Med Chem (2018) 156 : 93 -102
PubMed 30006177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.42 4.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1438938 1 4.64
CHEMBL449635 1 4.19
CHEMBL4287262 1 -
CHEMBL4287655 1 -
CHEMBL4208737 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1438938 IC50 = 23000.0 nM 4.64
CHEMBL449635 IC50 = 65000.0 nM 4.19
CHEMBL4287262 IC50 > 100000.0 nM -
CHEMBL4287655 IC50 > 100000.0 nM -
CHEMBL4208737 IC50 > 100000.0 nM -