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Assay Detail

CHEMBL4617152

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

Binding
Inhibition of recombinant human PARG assessed as mono(ADP-R) release using PAR as substrate measured after 15 mins by HPLC analysis
5
Total Activities
5
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) glycohydrolase (CHEMBL1795143)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural insights into the active site of poly(ADP-ribose) glycohydrolase using docking modes of 6-hydroxy-3H-xanthen-3-one derivative inhibitors.
Shibui Y, Oyama T, Okazawa M, Yoshimori A, Abe H, Uchiumi F, Tanuma SI.
Bioorg Med Chem (2020) 28 : 115249 -115249
PubMed 31879180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.37 4.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1208422 ROSE BENGAL FREE ACID 4.0 1 4.53
CHEMBL1254258 1 4.21
CHEMBL5483017 1 -
CHEMBL376503 1 -
CHEMBL1205178 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1208422 ROSE BENGAL FREE ACID IC50 = 29700.0 nM 4.53
CHEMBL1254258 IC50 = 61400.0 nM 4.21
CHEMBL5483017 IC50 = 120100.0 nM -
CHEMBL376503 IC50 > 300000.0 nM -
CHEMBL1205178 IC50 = 105600.0 nM -