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Assay Detail

CHEMBL4312178

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

Binding
Inhibition of human recombinant SIRT1 using p53 (379 to 382 residues) conjugated to AMC as substrate incubated for 45 mins in presence of NAD+ by fluorescence assay
8
Total Activities
8
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

Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives.
Yeong KY, Nor Azizi MIH, Berdigaliyev N, Chen WN, Lee WL, Shirazi AN, Parang K.
Medchemcomm (2019) 10 : 2140 -2145
PubMed 32904142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.12 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420311 1 6.52
CHEMBL4446030 1 5.11
CHEMBL4536622 1 4.47
CHEMBL595354 1 4.38
CHEMBL4520707 1 -
CHEMBL4469996 1 -
CHEMBL4452096 1 -
CHEMBL224864 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420311 IC50 = 300.0 nM 6.52
CHEMBL4446030 IC50 = 7700.0 nM 5.11
CHEMBL4536622 IC50 = 33600.0 nM 4.47
CHEMBL595354 IC50 = 42100.0 nM 4.38
CHEMBL4520707 IC50 > 50000.0 nM -
CHEMBL4469996 IC50 > 50000.0 nM -
CHEMBL4452096 IC50 > 50000.0 nM -
CHEMBL224864 IC50 - -