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Assay Detail

CHEMBL3619957

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Binding
Inhibition of PARP1 (unknown origin)
14
Total Activities
14
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

Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.
Xie Z, Zhou Y, Zhao W, Jiao H, Chen Y, Yang Y, Li Z.
Bioorg Med Chem Lett (2015) 25 : 4557 -4561
PubMed 26342868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.97 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173055 RUCAPARIB 4.0 1 9.10
CHEMBL3617774 1 8.62
CHEMBL3617773 1 8.46
CHEMBL3617772 1 8.18
CHEMBL3617778 1 7.45
CHEMBL3617776 1 6.86
CHEMBL3617771 1 6.60
CHEMBL3617777 1 6.33
CHEMBL3617768 1 5.57
CHEMBL3617770 1 4.95
CHEMBL81977 3-AMINOBENZAMIDE 1 4.52
CHEMBL3617775 1 -
CHEMBL3617769 1 -
CHEMBL1140 NIACINAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173055 RUCAPARIB IC50 = 0.8044 nM 9.10
CHEMBL3617774 IC50 = 2.416 nM 8.62
CHEMBL3617773 IC50 = 3.501 nM 8.46
CHEMBL3617772 IC50 = 6.643 nM 8.18
CHEMBL3617778 IC50 = 35.44 nM 7.45
CHEMBL3617776 IC50 = 137.6 nM 6.86
CHEMBL3617771 IC50 = 249.7 nM 6.60
CHEMBL3617777 IC50 = 465.4 nM 6.33
CHEMBL3617768 IC50 = 2697.0 nM 5.57
CHEMBL3617770 IC50 = 11292.0 nM 4.95
CHEMBL81977 3-AMINOBENZAMIDE IC50 = 30000.0 nM 4.52
CHEMBL3617775 IC50 = 2.952 10'8nM -
CHEMBL3617769 IC50 = 6.076 10'13nM -
CHEMBL1140 NIACINAMIDE IC50 = 210000.0 nM -