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Assay Detail

CHEMBL4190587

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

Binding
Inhibition of human recombinant SIRT1 using AMC-p53 (379 to 382 residues) as substrate incubated for 45 mins followed by NAD+ addition measured after 30 mins by fluorescence assay
12
Total Activities
12
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

NAD-dependent protein deacetylase sirtuin-1 (CHEMBL4506)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Medchemcomm (2016) 7 : 2094 -2099
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.86 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420311 1 6.52
CHEMBL4216715 1 4.99
CHEMBL4202895 1 4.70
CHEMBL4210076 1 4.53
CHEMBL4212277 1 4.46
CHEMBL4214892 1 4.43
CHEMBL595354 1 4.38
CHEMBL4217034 1 -
CHEMBL224864 1 -
CHEMBL4211748 1 -
CHEMBL4218670 1 -
CHEMBL4218205 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420311 IC50 = 300.0 nM 6.52
CHEMBL4216715 IC50 = 10220.0 nM 4.99
CHEMBL4202895 IC50 = 19960.0 nM 4.70
CHEMBL4210076 IC50 = 29800.0 nM 4.53
CHEMBL4212277 IC50 = 35070.0 nM 4.46
CHEMBL4214892 IC50 = 36970.0 nM 4.43
CHEMBL595354 IC50 = 42100.0 nM 4.38
CHEMBL4217034 IC50 > 50000.0 nM -
CHEMBL224864 IC50 - -
CHEMBL4211748 IC50 > 50000.0 nM -
CHEMBL4218670 IC50 > 50000.0 nM -
CHEMBL4218205 IC50 > 50000.0 nM -