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Literature summary for 3.2.1.143 extracted from

  • Finch, K.E.; Knezevic, C.E.; Nottbohm, A.C.; Partlow, K.C.; Hergenrother, P.J.
    Selective small molecule inhibition of poly(ADP-ribose) glycohydrolase (PARG) (2012), ACS Chem. Biol., 7, 563-570.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.2.1.143

Inhibitors

Inhibitors Comment Organism Structure
(3Z)-5-bromo-1-(2,6-dichlorobenzyl)-3-[4-oxo-3-[2-(1H-tetrazol-5-yl)ethyl]-2-thioxo-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one specific detergent-insensitive inhibition Homo sapiens
(3Z)-5-chloro-1-(2,6-dichlorobenzyl)-3-[4-oxo-3-[2-(1H-tetrazol-5-yl)ethyl]-2-thioxo-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one specific detergent-insensitive inhibition Homo sapiens
3-[(5Z)-5-[1-(2-chlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid specific detergent-insensitive inhibition Homo sapiens
3-[(5Z)-5-[5-bromo-1-(2,6-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid specific detergent-insensitive inhibition Homo sapiens
3-[(5Z)-5-[5-bromo-1-(2-chloro-6-fluorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid specific detergent-insensitive inhibition Homo sapiens
3-[(5Z)-5-[5-chloro-1-(2,6-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid specific detergent-insensitive inhibition Homo sapiens
adenosine diphosphate (hydroxymethyl) pyrrolidinediol 39% inhibition at 0.025 mM Homo sapiens
Congo red detergent-sensitive inhibition with complete loss of inhibition in the presence of detergent Homo sapiens
additional information small molecule inhibitor screening, detection of rhodamine-based enzyme inhibitors (RBPIs), 3-[(5Z)-5-[1-(2-fluorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid and (3Z)-1-(2-fluorobenzyl)-3-[4-oxo-3-[2-(1H-tetrazol-5-yl)ethyl]-2-thioxo-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one are inactive, RBPIs do not inhibit beta-lactamase, ADP-ribosylhydrolase 3, or poly(ADP-ribose) polymerase 1. No inhibiiton by DMO Homo sapiens
salicylanilides
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
PARG
-
 Homo sapiens
poly(ADP-ribose) glycohydrolase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0029
-
 pH not specified in the publication, 37°C Homo sapiens 3-[(5Z)-5-[5-bromo-1-(2,6-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
0.003
-
 pH not specified in the publication, 37°C Homo sapiens 3-[(5Z)-5-[5-bromo-1-(2-chloro-6-fluorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
0.0045
-
 pH not specified in the publication, 37°C Homo sapiens (3Z)-5-bromo-1-(2,6-dichlorobenzyl)-3-[4-oxo-3-[2-(1H-tetrazol-5-yl)ethyl]-2-thioxo-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one
0.0058
-
 pH not specified in the publication, 37°C Homo sapiens 3-[(5Z)-5-[5-chloro-1-(2,6-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
0.0123
-
 pH not specified in the publication, 37°C Homo sapiens (3Z)-5-chloro-1-(2,6-dichlorobenzyl)-3-[4-oxo-3-[2-(1H-tetrazol-5-yl)ethyl]-2-thioxo-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one
0.0465
-
 pH not specified in the publication, 37°C Homo sapiens 3-[(5Z)-5-[1-(2-chlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid