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Assay Detail

CHEMBL859247

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Binding
Inhibitory activity against human PARP1 expressed in PC12 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-12
Confidence 9 — Direct single protein target
Curated By Expert

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Tao M, Park CH, Bihovsky R, Wells GJ, Husten J, Ator MA, Hudkins RL.
Bioorg Med Chem Lett (2006) 16 : 938 -942
PubMed 16290935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.03 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338790 1 7.58
CHEMBL204250 1 7.44
CHEMBL201907 1 7.40
CHEMBL201931 1 7.05
CHEMBL380809 1 6.16
CHEMBL373066 1 6.12
CHEMBL380940 1 5.70
CHEMBL381280 1 5.65
CHEMBL201723 1 5.30
CHEMBL381303 1 5.00
CHEMBL202426 1 5.00
CHEMBL370869 1 5.00
CHEMBL202537 1 5.00
CHEMBL201728 1 -
CHEMBL381460 1 -
CHEMBL383830 1 -
CHEMBL421087 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338790 IC50 = 26.0 nM 7.58
CHEMBL204250 IC50 = 36.0 nM 7.44
CHEMBL201907 IC50 = 40.0 nM 7.40
CHEMBL201931 IC50 = 90.0 nM 7.05
CHEMBL380809 IC50 = 700.0 nM 6.16
CHEMBL373066 IC50 = 750.0 nM 6.12
CHEMBL380940 IC50 = 2000.0 nM 5.70
CHEMBL381280 IC50 = 2220.0 nM 5.65
CHEMBL201723 IC50 = 5000.0 nM 5.30
CHEMBL381303 IC50 = 10000.0 nM 5.00
CHEMBL202426 IC50 = 10000.0 nM 5.00
CHEMBL370869 IC50 = 10000.0 nM 5.00
CHEMBL202537 IC50 = 10000.0 nM 5.00
CHEMBL201728 IC50 > 10000.0 nM -
CHEMBL381460 IC50 > 10000.0 nM -
CHEMBL383830 IC50 > 10000.0 nM -
CHEMBL421087 IC50 > 10000.0 nM -