Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1067345

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

Binding
Inhibition of human full length SIRT1 expressed in DE3 cells by fluorimetric assay
15
Total Activities
15
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

Identification and characterization of novel sirtuin inhibitor scaffolds.
Sanders BD, Jackson B, Brent M, Taylor AM, Dang W, Berger SL, Schreiber SL, Howitz K, Marmorstein R.
Bioorg Med Chem (2009) 17 : 7031 -7041
PubMed 19734050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.19 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446446 1 6.75
CHEMBL265502 SURAMIN 3.0 1 6.22
CHEMBL611953 1 6.19
CHEMBL595128 1 5.22
CHEMBL6291 BISINDOLYLMALEIMIDE IX 1 4.60
CHEMBL594863 1 4.47
CHEMBL82949 1 4.10
CHEMBL595354 1 4.00
CHEMBL592963 1 -
CHEMBL1140 NIACINAMIDE 4.0 1 -
CHEMBL380797 SIRTINOL 1 -
CHEMBL611614 1 -
CHEMBL86537 SPLITOMICIN 1 -
CHEMBL491960 CAMBINOL 1 -
CHEMBL508272 SURFACTIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446446 IC50 = 180.0 nM 6.75
CHEMBL265502 SURAMIN IC50 = 600.0 nM 6.22
CHEMBL611953 IC50 = 640.0 nM 6.19
CHEMBL595128 IC50 = 6000.0 nM 5.22
CHEMBL6291 BISINDOLYLMALEIMIDE IX IC50 = 25000.0 nM 4.60
CHEMBL594863 IC50 = 34000.0 nM 4.47
CHEMBL82949 IC50 = 80000.0 nM 4.10
CHEMBL595354 IC50 = 100000.0 nM 4.00
CHEMBL592963 IC50 = 570000.0 nM -
CHEMBL1140 NIACINAMIDE IC50 = 250000.0 nM -
CHEMBL380797 SIRTINOL IC50 = 120000.0 nM -
CHEMBL611614 IC50 - -
CHEMBL86537 SPLITOMICIN IC50 > 500000.0 nM -
CHEMBL491960 CAMBINOL IC50 > 600000.0 nM -
CHEMBL508272 SURFACTIN IC50 > 600000.0 nM -