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Assay Detail

CHEMBL4322644

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ADMET
Inhibition of human sirtuin 2 (25 to 389 residues) assessed as inhibition of substrate deacetylation using ZMAL as substrate incubated for 4 hrs by fluorescene-based analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from Schistosoma mansoni (SmSirt2).
Monaldi D, Rotili D, Lancelot J, Marek M, Wössner N, Lucidi A, Tomaselli D, Ramos-Morales E, Romier C, Pierce RJ, Mai A, Jung M.
J Med Chem (2019) 62 : 8733 -8759
PubMed 31496251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.92 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.40
CHEMBL3769988 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 400.0 nM 6.40
CHEMBL3769988 IC50 = 3700.0 nM 5.43