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Assay Detail

CHEMBL2341185

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

Binding
Inhibition of human recombinant ARTD1 by fluorescence assay
18
Total Activities
10
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

Screening and structural analysis of flavones inhibiting tankyrases.
Narwal M, Haikarainen T, Fallarero A, Vuorela PM, Lehtiö L.
J Med Chem (2013) 56 : 3507 -3517
PubMed 23574272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.23 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222556 2 5.90
CHEMBL275638 FLAVONE 2.0 2 5.86
CHEMBL147552 2 5.62
CHEMBL151 LUTEOLIN 2.0 2 5.38
CHEMBL301624 2 5.12
CHEMBL253786 2 5.02
CHEMBL53738 2 5.00
CHEMBL16861 2 4.60
CHEMBL28 APIGENIN 1 4.00
CHEMBL16751 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222556 IC50 = 1258.93 nM 5.90
CHEMBL222556 IC50 = 1300.0 nM 5.89
CHEMBL275638 FLAVONE IC50 = 1380.38 nM 5.86
CHEMBL275638 FLAVONE IC50 = 1400.0 nM 5.85
CHEMBL147552 IC50 = 2400.0 nM 5.62
CHEMBL147552 IC50 = 2454.71 nM 5.61
CHEMBL151 LUTEOLIN IC50 = 4200.0 nM 5.38
CHEMBL151 LUTEOLIN IC50 = 4265.8 nM 5.37
CHEMBL301624 IC50 = 7585.78 nM 5.12
CHEMBL301624 IC50 = 7500.0 nM 5.12
CHEMBL253786 IC50 = 9549.93 nM 5.02
CHEMBL253786 IC50 = 9500.0 nM 5.02
CHEMBL53738 IC50 = 9900.0 nM 5.00
CHEMBL53738 IC50 = 10000.0 nM 5.00
CHEMBL16861 IC50 = 25000.0 nM 4.60
CHEMBL16861 IC50 = 25703.96 nM 4.59
CHEMBL28 APIGENIN IC50 = 100000.0 nM 4.00
CHEMBL16751 IC50 > 100000.0 nM -