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Assay Detail

CHEMBL5361128

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Binding
Inhibition of human SIRT5
9
Total Activities
9
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

Pyrazolone derivatives as potent and selective small-molecule SIRT5 inhibitors.
Yao J, Yin Y, Han H, Chen S, Zheng Y, Liang B, Wu M, Shu K, Debnath B, Lombard DB, Wang Q, Cheng K, Neamati N, Liu Y.
Eur J Med Chem (2023) 247 : 115024 -115024
PubMed 36543033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.74 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636862 1 6.96
CHEMBL5182606 1 6.47
CHEMBL5199472 1 5.66
CHEMBL5187910 1 5.60
CHEMBL4875043 1 5.52
CHEMBL1201346 BALSALAZIDE 4.0 1 5.28
CHEMBL4072635 1 5.25
CHEMBL5204662 1 5.14
CHEMBL5199270 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636862 IC50 = 110.0 nM 6.96
CHEMBL5182606 IC50 = 340.0 nM 6.47
CHEMBL5199472 IC50 = 2200.0 nM 5.66
CHEMBL5187910 IC50 = 2500.0 nM 5.60
CHEMBL4875043 IC50 = 3000.0 nM 5.52
CHEMBL1201346 BALSALAZIDE IC50 = 5300.0 nM 5.28
CHEMBL4072635 IC50 = 5600.0 nM 5.25
CHEMBL5204662 IC50 = 7200.0 nM 5.14
CHEMBL5199270 IC50 <= 50.0 nM -