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Assay Detail

CHEMBL4122798

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

Binding
Inhibition of full length recombinant His6-tagged human PARP1 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
5
Total Activities
4
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

Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.
Holechek J, Lease R, Thorsell AG, Karlberg T, McCadden C, Grant R, Keen A, Callahan E, Schüler H, Ferraris D.
Bioorg Med Chem Lett (2018) 28 : 2050 -2054
PubMed 29748053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.72 4.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4129001 2 4.72
CHEMBL1438938 1 -
CHEMBL4129789 1 -
CHEMBL4125748 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4129001 IC50 = 19000.0 nM 4.72
CHEMBL4129001 IC50 = 19054.61 nM 4.72
CHEMBL1438938 IC50 > 100000.0 nM -
CHEMBL4129789 IC50 > 100000.0 nM -
CHEMBL4125748 IC50 > 100000.0 nM -