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Assay Detail

CHEMBL2209185

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Binding
Inhibition of SIRT5 using ZK(suc)A substrate after 1 hr by homogeneous fluorescence assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Inhibitors of the NAD(+)-Dependent Protein Desuccinylase and Demalonylase Sirt5.
Maurer B, Rumpf T, Scharfe M, Stolfa DA, Schmitt ML, He W, Verdin E, Sippl W, Jung M.
ACS Med Chem Lett (2012) 3 : 1050 -1053
PubMed 24900427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.67 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203548 1 5.64
CHEMBL2203547 1 5.44
CHEMBL2203543 1 5.21
CHEMBL2203544 1 4.91
CHEMBL1715925 1 4.90
CHEMBL2203541 1 4.89
CHEMBL2203539 1 4.78
CHEMBL2203540 1 4.75
CHEMBL2203546 1 4.65
CHEMBL2203537 1 4.57
CHEMBL1795371 1 4.52
CHEMBL2203545 1 4.41
CHEMBL491960 CAMBINOL 1 4.37
CHEMBL1714005 1 4.33
CHEMBL1140 NIACINAMIDE 4.0 1 4.33
CHEMBL265502 SURAMIN 3.0 1 4.33
CHEMBL380797 SIRTINOL 1 4.31
CHEMBL2203538 1 4.25
CHEMBL2203542 1 4.17
CHEMBL1591531 1 -
CHEMBL420311 1 -
CHEMBL270292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203548 IC50 = 2300.0 nM 5.64
CHEMBL2203547 IC50 = 3600.0 nM 5.44
CHEMBL2203543 IC50 = 6200.0 nM 5.21
CHEMBL2203544 IC50 = 12400.0 nM 4.91
CHEMBL1715925 IC50 = 12600.0 nM 4.90
CHEMBL2203541 IC50 = 12900.0 nM 4.89
CHEMBL2203539 IC50 = 16600.0 nM 4.78
CHEMBL2203540 IC50 = 17800.0 nM 4.75
CHEMBL2203546 IC50 = 22400.0 nM 4.65
CHEMBL2203537 IC50 = 27000.0 nM 4.57
CHEMBL1795371 IC50 = 30000.0 nM 4.52
CHEMBL2203545 IC50 = 39400.0 nM 4.41
CHEMBL491960 CAMBINOL IC50 = 42500.0 nM 4.37
CHEMBL1714005 IC50 = 46500.0 nM 4.33
CHEMBL1140 NIACINAMIDE IC50 = 46600.0 nM 4.33
CHEMBL265502 SURAMIN IC50 = 46600.0 nM 4.33
CHEMBL380797 SIRTINOL IC50 = 48900.0 nM 4.31
CHEMBL2203538 IC50 = 55900.0 nM 4.25
CHEMBL2203542 IC50 = 67300.0 nM 4.17
CHEMBL1591531 IC50 - -
CHEMBL420311 IC50 - -
CHEMBL270292 IC50 - -