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Assay Detail

CHEMBL1010816

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Binding
Inhibition of human recombinant PARP2
6
Total Activities
6
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 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.
J Med Chem (2009) 52 : 514 -523
PubMed 19143569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.46 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497608 1 8.70
CHEMBL526668 1 8.70
CHEMBL495942 1 8.70
CHEMBL495743 1 8.40
CHEMBL506871 VELIPARIB 3.0 1 8.30
CHEMBL527654 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497608 Ki = 2.0 nM 8.70
CHEMBL526668 Ki = 2.0 nM 8.70
CHEMBL495942 Ki = 2.0 nM 8.70
CHEMBL495743 Ki = 4.0 nM 8.40
CHEMBL506871 VELIPARIB Ki = 5.0 nM 8.30
CHEMBL527654 Ki = 11.0 nM 7.96