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Assay Detail

CHEMBL4156262

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

Binding
Inhibition of recombinant His-tagged SIRT2 (56 to 356 residues) (unknown origin) expressed in Escherichia coli Transetta(DE3) using AcIQF as substrate preincubated for 30 mins followed by substrate and NAD+ addition measured after 2 hrs by fluorescence assay
ChEMBL ↗
80
Total Activities
40
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-2 (CHEMBL4462) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.
Yang LL, Wang HL, Zhong L, Yuan C, Liu SY, Yu ZJ, Liu S, Yan YH, Wu C, Wang Y, Wang Z, Yu Y, Chen Q, Li GB.
Eur J Med Chem (2018) 155 : 806 -823
PubMed 29957526 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 4.81 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170094 — — 2 6.09
CHEMBL4171986 — — 2 5.88
CHEMBL4161780 — — 2 5.51
CHEMBL4070149 — — 2 5.47
CHEMBL3770903 — — 2 5.47
CHEMBL4176673 — — 2 5.02
CHEMBL4169477 — — 2 4.93
CHEMBL4167005 — — 2 4.82
CHEMBL4079934 — — 2 4.59
CHEMBL4173548 — — 2 4.53
CHEMBL4171455 — — 2 4.38
CHEMBL4175593 — — 2 4.35
CHEMBL4161556 — — 2 4.15
CHEMBL4174893 — — 2 4.12
CHEMBL4170003 — — 2 4.05
CHEMBL4159477 — — 2 4.03
CHEMBL4159773 — — 2 4.00
CHEMBL4164971 — — 2 -
CHEMBL4170414 — — 2 -
CHEMBL4160877 — — 2 -
CHEMBL4172158 — — 2 -
CHEMBL4164275 — — 2 -
CHEMBL4167724 — — 2 -
CHEMBL4160492 — — 2 -
CHEMBL4171097 — — 2 -
CHEMBL4173707 — — 2 -
CHEMBL4165789 — — 2 -
CHEMBL4163136 — — 2 -
CHEMBL4176250 — — 2 -
CHEMBL4168392 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170094 — IC50 = 812.83 nM 6.09
CHEMBL4170094 — IC50 = 815.0 nM 6.09
CHEMBL4171986 — IC50 = 1318.26 nM 5.88
CHEMBL4171986 — IC50 = 1320.0 nM 5.88
CHEMBL4161780 — IC50 = 3100.0 nM 5.51
CHEMBL4161780 — IC50 = 3090.3 nM 5.51
CHEMBL3770903 — IC50 = 3380.0 nM 5.47
CHEMBL3770903 — IC50 = 3388.44 nM 5.47
CHEMBL4070149 — IC50 = 3410.0 nM 5.47
CHEMBL4070149 — IC50 = 3388.44 nM 5.47
CHEMBL4176673 — IC50 = 9560.0 nM 5.02
CHEMBL4176673 — IC50 = 9549.93 nM 5.02
CHEMBL4169477 — IC50 = 11748.98 nM 4.93
CHEMBL4169477 — IC50 = 11700.0 nM 4.93
CHEMBL4167005 — IC50 = 15135.61 nM 4.82
CHEMBL4167005 — IC50 = 15200.0 nM 4.82
CHEMBL4079934 — IC50 = 25900.0 nM 4.59
CHEMBL4079934 — IC50 = 26302.68 nM 4.58
CHEMBL4173548 — IC50 = 29512.09 nM 4.53
CHEMBL4173548 — IC50 = 29400.0 nM 4.53
CHEMBL4171455 — IC50 = 41300.0 nM 4.38
CHEMBL4171455 — IC50 = 41686.94 nM 4.38
CHEMBL4175593 — IC50 = 44450.0 nM 4.35
CHEMBL4175593 — IC50 = 44668.36 nM 4.35
CHEMBL4161556 — IC50 = 70600.0 nM 4.15
CHEMBL4161556 — IC50 = 70794.58 nM 4.15
CHEMBL4174893 — IC50 = 75857.76 nM 4.12
CHEMBL4174893 — IC50 = 76100.0 nM 4.12
CHEMBL4170003 — IC50 = 89125.09 nM 4.05
CHEMBL4170003 — IC50 = 89300.0 nM 4.05
CHEMBL4159477 — IC50 = 93325.43 nM 4.03
CHEMBL4159477 — IC50 = 93700.0 nM 4.03
CHEMBL4159773 — IC50 = 100000.0 nM 4.00
CHEMBL4173707 — IC50 > 300000.0 nM -
CHEMBL4171097 — IC50 > 301995.17 nM -
CHEMBL4171097 — IC50 > 300000.0 nM -
CHEMBL4160492 — IC50 > 301995.17 nM -
CHEMBL4160492 — IC50 > 300000.0 nM -
CHEMBL4163136 — IC50 > 300000.0 nM -
CHEMBL4167724 — IC50 > 300000.0 nM -
CHEMBL4176250 — IC50 = 301995.17 nM -
CHEMBL4164971 — IC50 > 300000.0 nM -
CHEMBL4164971 — IC50 > 301995.17 nM -
CHEMBL4160877 — IC50 > 300000.0 nM -
CHEMBL4160877 — IC50 > 301995.17 nM -
CHEMBL4172158 — IC50 = 141600.0 nM -
CHEMBL4164275 — IC50 = 269153.48 nM -
CHEMBL4164275 — IC50 = 269700.0 nM -
CHEMBL4172158 — IC50 = 141253.75 nM -
CHEMBL4167724 — IC50 > 301995.17 nM -