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Assay Detail

CHEMBL1814965

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Binding
Inhibition of PARP-1 using [32P]-NAD+ after 15 mins
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).
Steffen JD, Coyle DL, Damodaran K, Beroza P, Jacobson MK.
J Med Chem (2011) 54 : 5403 -5413
PubMed 21692479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.56 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267373 BENZAMIDE 1 5.27
CHEMBL115114 1 4.66
CHEMBL1813887 1 4.18
CHEMBL1813880 1 4.11
CHEMBL1813879 1 -
CHEMBL1813881 1 -
CHEMBL1814050 1 -
CHEMBL1814051 1 -
CHEMBL1230692 ADENOSINE DIPHOSPHATE (HYDROXYMETHYL)PYRROLIDINEDIOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267373 BENZAMIDE IC50 = 5400.0 nM 5.27
CHEMBL115114 IC50 = 22000.0 nM 4.66
CHEMBL1813887 IC50 = 66000.0 nM 4.18
CHEMBL1813880 IC50 = 78000.0 nM 4.11
CHEMBL1813879 IC50 = 123000.0 nM -
CHEMBL1813881 IC50 = 120000.0 nM -
CHEMBL1814050 IC50 = 500000.0 nM -
CHEMBL1814051 IC50 = 500000.0 nM -
CHEMBL1230692 ADENOSINE DIPHOSPHATE (HYDROXYMETHYL)PYRROLIDINEDIOL IC50 > 1000000.0 nM -