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Assay Detail

CHEMBL992764

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Binding
Inhibition of PARP2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Poly [ADP-ribose] polymerase 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL.
Bioorg Med Chem (2008) 16 : 6965 -6975
PubMed 18541433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.22 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452801 1 8.70
CHEMBL460267 1 8.52
CHEMBL452800 1 8.30
CHEMBL527654 1 7.96
CHEMBL518484 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452801 Ki = 2.0 nM 8.70
CHEMBL460267 Ki = 3.0 nM 8.52
CHEMBL452800 Ki = 5.0 nM 8.30
CHEMBL527654 Ki = 11.0 nM 7.96
CHEMBL518484 Ki = 24.0 nM 7.62