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Assay Detail

CHEMBL762474

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Concentration required to inhibit human recombinant PARP-1 was determined using cell protection assay
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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
EC50 30 6.59 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108840 1 7.16
CHEMBL108339 2 7.16
CHEMBL322133 1 7.16
CHEMBL108702 1 7.16
CHEMBL433356 1 7.10
CHEMBL323488 1 7.10
CHEMBL321703 1 7.00
CHEMBL108623 1 7.00
CHEMBL430707 1 7.00
CHEMBL107601 1 7.00
CHEMBL419020 1 7.00
CHEMBL108919 1 7.00
CHEMBL107764 1 6.70
CHEMBL110115 1 6.70
CHEMBL321638 1 6.70
CHEMBL107260 1 6.52
CHEMBL108239 1 6.40
CHEMBL108137 1 6.40
CHEMBL111606 1 6.30
CHEMBL108968 1 6.30
CHEMBL107935 1 6.30
CHEMBL108341 1 6.30
CHEMBL108316 1 6.22
CHEMBL410733 1 6.16
CHEMBL432211 1 6.10
CHEMBL421605 1 6.05
CHEMBL107616 1 5.70
CHEMBL322957 1 5.46
CHEMBL110178 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108840 EC50 = 70.0 nM 7.16
CHEMBL108339 EC50 = 70.0 nM 7.16
CHEMBL322133 EC50 = 70.0 nM 7.16
CHEMBL108702 EC50 = 70.0 nM 7.16
CHEMBL433356 EC50 = 80.0 nM 7.10
CHEMBL323488 EC50 = 80.0 nM 7.10
CHEMBL321703 EC50 = 100.0 nM 7.00
CHEMBL108623 EC50 = 100.0 nM 7.00
CHEMBL430707 EC50 = 100.0 nM 7.00
CHEMBL107601 EC50 = 100.0 nM 7.00
CHEMBL419020 EC50 = 100.0 nM 7.00
CHEMBL108919 EC50 = 100.0 nM 7.00
CHEMBL321638 EC50 = 200.0 nM 6.70
CHEMBL110115 EC50 = 200.0 nM 6.70
CHEMBL107764 EC50 = 200.0 nM 6.70
CHEMBL107260 EC50 = 300.0 nM 6.52
CHEMBL108239 EC50 = 400.0 nM 6.40
CHEMBL108137 EC50 = 400.0 nM 6.40
CHEMBL111606 EC50 = 500.0 nM 6.30
CHEMBL108968 EC50 = 500.0 nM 6.30
CHEMBL107935 EC50 = 500.0 nM 6.30
CHEMBL108341 EC50 = 500.0 nM 6.30
CHEMBL108316 EC50 = 600.0 nM 6.22
CHEMBL410733 EC50 = 700.0 nM 6.16
CHEMBL432211 EC50 = 800.0 nM 6.10
CHEMBL108339 EC50 = 800.0 nM 6.10
CHEMBL421605 EC50 = 900.0 nM 6.05
CHEMBL107616 EC50 = 2000.0 nM 5.70
CHEMBL322957 EC50 = 3500.0 nM 5.46
CHEMBL110178 EC50 > 1000.0 nM -