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Assay Detail

CHEMBL4185229

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

Binding
Inhibition of N-terminal His6-tagged recombinant Leishmania infantum SIR2RP1 expressed in Escherichia coli in presence of NAD+ by fluorimetric method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Leishmania infantum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Putative silent information regulator 2 (CHEMBL2311240)
Type SINGLE PROTEIN
Organism Leishmania infantum

Publication

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
Hailu GS, Robaa D, Forgione M, Sippl W, Rotili D, Mai A.
J Med Chem (2017) 60 : 4780 -4804
PubMed 28241112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.18 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4216559 1 5.24
CHEMBL4211052 1 5.24
CHEMBL4204117 1 5.24
CHEMBL4215363 1 5.24
CHEMBL4206570 1 5.24
CHEMBL4211460 1 5.24
CHEMBL4214749 1 5.24
CHEMBL4209842 1 5.24
CHEMBL4217062 1 5.24
CHEMBL4205463 1 5.24
CHEMBL4205986 1 5.24
CHEMBL4217704 1 5.24
CHEMBL4218232 1 5.24
CHEMBL265502 SURAMIN 3.0 1 5.16
CHEMBL1140 NIACINAMIDE 4.0 1 4.40
CHEMBL380797 SIRTINOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4216559 IC50 = 5700.0 nM 5.24
CHEMBL4211052 IC50 = 5700.0 nM 5.24
CHEMBL4204117 IC50 = 5700.0 nM 5.24
CHEMBL4215363 IC50 = 5700.0 nM 5.24
CHEMBL4206570 IC50 = 5700.0 nM 5.24
CHEMBL4211460 IC50 = 5700.0 nM 5.24
CHEMBL4214749 IC50 = 5700.0 nM 5.24
CHEMBL4209842 IC50 = 5700.0 nM 5.24
CHEMBL4217062 IC50 = 5700.0 nM 5.24
CHEMBL4205463 IC50 = 5700.0 nM 5.24
CHEMBL4205986 IC50 = 5700.0 nM 5.24
CHEMBL4217704 IC50 = 5700.0 nM 5.24
CHEMBL4218232 IC50 = 5700.0 nM 5.24
CHEMBL265502 SURAMIN IC50 = 7000.0 nM 5.16
CHEMBL1140 NIACINAMIDE IC50 = 40000.0 nM 4.40
CHEMBL380797 SIRTINOL IC50 = 194000.0 nM -