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Assay Detail

CHEMBL3595281

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

Binding
Inhibition of full-length human ARTD1 using 500 nM NAD substrate after 1 hr incubation
4
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

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.
Nkizinkiko Y, Suneel Kumar BV, Jeankumar VU, Haikarainen T, Koivunen J, Madhuri C, Yogeeswari P, Venkannagari H, Obaji E, Pihlajaniemi T, Sriram D, Lehtiö L.
Bioorg Med Chem (2015) 23 : 4139 -4149
PubMed 26183543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.34 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3593716 1 5.44
CHEMBL3593715 1 5.23
CHEMBL3594137 1 -
CHEMBL3594136 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3593716 IC50 = 3600.0 nM 5.44
CHEMBL3593715 IC50 = 5900.0 nM 5.23
CHEMBL3594137 IC50 > 100000.0 nM -
CHEMBL3594136 IC50 > 100000.0 nM -