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Assay Detail

CHEMBL4353606

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

Binding
Inhibition of human N-terminal His-tagged SIRT3 (102 to 399 residues) expressed in Escherichia coli using p53 (Gln-Pro-Lys-Lys(Ac)) (317 to 320 residues) as substrate incubated for 3 hrs measured up to 30 mins by fluorescence assay
1
Total Activities
1
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

Publication

Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD<sup>+</sup>-Binding Site.
Mellini P, Itoh Y, Elboray EE, Tsumoto H, Li Y, Suzuki M, Takahashi Y, Tojo T, Kurohara T, Miyake Y, Miura Y, Kitao Y, Kotoku M, Iida T, Suzuki T.
J Med Chem (2019) 62 : 5844 -5862
PubMed 31144814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.16 4.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465620 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465620 IC50 = 69200.0 nM 4.16