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Assay Detail

CHEMBL859693

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Binding
Inhibitory activity against human SIRT1 by radiochemical Nicotinamide release assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1.
Napper AD, Hixon J, McDonagh T, Keavey K, Pons JF, Barker J, Yau WT, Amouzegh P, Flegg A, Hamelin E, Thomas RJ, Kates M, Jones S, Navia MA, Saunders JO, DiStefano PS, Curtis R.
J Med Chem (2005) 48 : 8045 -8054
PubMed 16335928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.79 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446446 1 6.19
CHEMBL420311 1 5.89
CHEMBL115600 1 5.60
CHEMBL112265 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446446 IC50 = 652.0 nM 6.19
CHEMBL420311 IC50 = 1290.0 nM 5.89
CHEMBL115600 IC50 = 2500.0 nM 5.60
CHEMBL112265 IC50 = 3300.0 nM 5.48