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Assay Detail

CHEMBL762476

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Binding
Inhibitory activity against human recombinant PARP-1
43
Total Activities
42
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 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Steinhagen H, Gerisch M, Mittendorf J, Schlemmer KH, Albrecht B.
Bioorg Med Chem Lett (2002) 12 : 3187 -3190
PubMed 12372530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.24 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323488 1 8.07
CHEMBL108919 1 7.92
CHEMBL107764 1 7.92
CHEMBL321638 1 7.82
CHEMBL322133 1 7.82
CHEMBL321703 1 7.82
CHEMBL108702 1 7.70
CHEMBL108239 1 7.70
CHEMBL107601 1 7.70
CHEMBL108341 1 7.70
CHEMBL108623 1 7.70
CHEMBL108339 2 7.70
CHEMBL433356 1 7.60
CHEMBL108840 1 7.60
CHEMBL108137 1 7.60
CHEMBL432211 1 7.60
CHEMBL108968 1 7.52
CHEMBL107935 1 7.52
CHEMBL110115 1 7.52
CHEMBL430707 1 7.46
CHEMBL110178 1 7.40
CHEMBL419020 1 7.40
CHEMBL108316 1 7.30
CHEMBL111606 1 7.22
CHEMBL320579 1 7.22
CHEMBL410733 1 7.16
CHEMBL107616 1 7.16
CHEMBL322957 1 7.16
CHEMBL421605 1 7.10
CHEMBL107260 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323488 IC50 = 8.5 nM 8.07
CHEMBL108919 IC50 = 12.0 nM 7.92
CHEMBL107764 IC50 = 12.0 nM 7.92
CHEMBL321638 IC50 = 15.0 nM 7.82
CHEMBL322133 IC50 = 15.0 nM 7.82
CHEMBL321703 IC50 = 15.0 nM 7.82
CHEMBL108702 IC50 = 20.0 nM 7.70
CHEMBL108239 IC50 = 20.0 nM 7.70
CHEMBL108339 IC50 = 20.0 nM 7.70
CHEMBL108623 IC50 = 20.0 nM 7.70
CHEMBL107601 IC50 = 20.0 nM 7.70
CHEMBL108341 IC50 = 20.0 nM 7.70
CHEMBL108840 IC50 = 25.0 nM 7.60
CHEMBL432211 IC50 = 25.0 nM 7.60
CHEMBL433356 IC50 = 25.0 nM 7.60
CHEMBL108339 IC50 = 25.0 nM 7.60
CHEMBL108137 IC50 = 25.0 nM 7.60
CHEMBL110115 IC50 = 30.0 nM 7.52
CHEMBL108968 IC50 = 30.0 nM 7.52
CHEMBL107935 IC50 = 30.0 nM 7.52
CHEMBL430707 IC50 = 35.0 nM 7.46
CHEMBL419020 IC50 = 40.0 nM 7.40
CHEMBL110178 IC50 = 40.0 nM 7.40
CHEMBL108316 IC50 = 50.0 nM 7.30
CHEMBL320579 IC50 = 60.0 nM 7.22
CHEMBL111606 IC50 = 60.0 nM 7.22
CHEMBL107616 IC50 = 70.0 nM 7.16
CHEMBL410733 IC50 = 70.0 nM 7.16
CHEMBL322957 IC50 = 70.0 nM 7.16
CHEMBL421605 IC50 = 80.0 nM 7.10
CHEMBL107260 IC50 = 90.0 nM 7.05
CHEMBL432406 IC50 = 150.0 nM 6.82
CHEMBL322268 IC50 = 200.0 nM 6.70
CHEMBL105765 IC50 = 250.0 nM 6.60
CHEMBL449084 IC50 = 300.0 nM 6.52
CHEMBL110681 IC50 = 400.0 nM 6.40
CHEMBL105925 IC50 = 450.0 nM 6.35
CHEMBL110332 IC50 = 800.0 nM 6.10
CHEMBL325336 IC50 = 900.0 nM 6.05
CHEMBL110729 IC50 = 900.0 nM 6.05
CHEMBL110682 IC50 = 3000.0 nM 5.52
CHEMBL110347 IC50 > 5000.0 nM -
CHEMBL326451 IC50 > 5000.0 nM -