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Assay Detail

CHEMBL1028889

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

Binding
Inhibition of human recombinant PARP1 by Trevigen colorimetric assay
17
Total Activities
17
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 in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Lord AM, Mahon MF, Lloyd MD, Threadgill MD.
J Med Chem (2009) 52 : 868 -877
PubMed 19117416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.31 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471966 1 6.30
CHEMBL526128 1 6.10
CHEMBL480429 1 6.05
CHEMBL481591 1 5.96
CHEMBL446240 1 5.75
CHEMBL502330 1 5.72
CHEMBL504903 1 5.66
CHEMBL501330 1 5.64
CHEMBL504998 1 5.47
CHEMBL453989 1 5.43
CHEMBL481793 1 5.24
CHEMBL450259 1 4.82
CHEMBL481803 1 4.64
CHEMBL480428 1 4.57
CHEMBL480427 1 4.37
CHEMBL479635 1 4.28
CHEMBL480233 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471966 IC50 = 500.0 nM 6.30
CHEMBL526128 IC50 = 800.0 nM 6.10
CHEMBL480429 IC50 = 900.0 nM 6.05
CHEMBL481591 IC50 = 1100.0 nM 5.96
CHEMBL446240 IC50 = 1800.0 nM 5.75
CHEMBL502330 IC50 = 1900.0 nM 5.72
CHEMBL504903 IC50 = 2200.0 nM 5.66
CHEMBL501330 IC50 = 2300.0 nM 5.64
CHEMBL504998 IC50 = 3400.0 nM 5.47
CHEMBL453989 IC50 = 3700.0 nM 5.43
CHEMBL481793 IC50 = 5800.0 nM 5.24
CHEMBL450259 IC50 = 15000.0 nM 4.82
CHEMBL481803 IC50 = 23000.0 nM 4.64
CHEMBL480428 IC50 = 27000.0 nM 4.57
CHEMBL480427 IC50 = 43000.0 nM 4.37
CHEMBL479635 IC50 = 52000.0 nM 4.28
CHEMBL480233 IC50 = 62000.0 nM 4.21