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Assay Detail

CHEMBL3773441

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

Binding
Inhibition of N-terminal his6-tagged human SIRT2 (25 to 389 amino acids) using ZMAL as substrate after 4 hrs by fluorescence-based microplate reader method
38
Total Activities
38
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

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study.
Schiedel M, Rumpf T, Karaman B, Lehotzky A, Oláh J, Gerhardt S, Ovádi J, Sippl W, Einsle O, Jung M.
J Med Chem (2016) 59 : 1599 -1612
PubMed 26696402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.52 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770049 1 6.75
CHEMBL3771286 1 6.68
CHEMBL3769991 1 6.58
CHEMBL3770797 1 6.51
CHEMBL3771296 1 6.50
CHEMBL3771164 1 6.38
CHEMBL3770903 1 6.36
CHEMBL3770258 1 6.32
CHEMBL3769999 1 6.27
CHEMBL3771278 1 6.27
CHEMBL3771012 1 5.88
CHEMBL3770983 1 5.84
CHEMBL3770654 1 5.79
CHEMBL3769691 1 5.72
CHEMBL3770429 1 5.72
CHEMBL3770426 1 5.63
CHEMBL3771035 1 5.47
CHEMBL3769988 1 5.43
CHEMBL3769677 1 5.33
CHEMBL3769518 1 5.01
CHEMBL3770872 1 4.84
CHEMBL3770811 1 4.82
CHEMBL3771302 1 4.78
CHEMBL3769473 1 4.70
CHEMBL3770731 1 4.51
CHEMBL3770857 1 4.48
CHEMBL3770860 1 4.48
CHEMBL3770553 1 4.34
CHEMBL3770486 1 4.19
CHEMBL3770474 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770049 IC50 = 180.0 nM 6.75
CHEMBL3771286 IC50 = 210.0 nM 6.68
CHEMBL3769991 IC50 = 260.0 nM 6.58
CHEMBL3770797 IC50 = 310.0 nM 6.51
CHEMBL3771296 IC50 = 320.0 nM 6.50
CHEMBL3771164 IC50 = 420.0 nM 6.38
CHEMBL3770903 IC50 = 440.0 nM 6.36
CHEMBL3770258 IC50 = 480.0 nM 6.32
CHEMBL3769999 IC50 = 540.0 nM 6.27
CHEMBL3771278 IC50 = 540.0 nM 6.27
CHEMBL3771012 IC50 = 1330.0 nM 5.88
CHEMBL3770983 IC50 = 1450.0 nM 5.84
CHEMBL3770654 IC50 = 1640.0 nM 5.79
CHEMBL3769691 IC50 = 1920.0 nM 5.72
CHEMBL3770429 IC50 = 1890.0 nM 5.72
CHEMBL3770426 IC50 = 2340.0 nM 5.63
CHEMBL3771035 IC50 = 3400.0 nM 5.47
CHEMBL3769988 IC50 = 3750.0 nM 5.43
CHEMBL3769677 IC50 = 4720.0 nM 5.33
CHEMBL3769518 IC50 = 9770.0 nM 5.01
CHEMBL3770872 IC50 = 14600.0 nM 4.84
CHEMBL3770811 IC50 = 15000.0 nM 4.82
CHEMBL3771302 IC50 = 16800.0 nM 4.78
CHEMBL3769473 IC50 = 19900.0 nM 4.70
CHEMBL3770731 IC50 = 30900.0 nM 4.51
CHEMBL3770857 IC50 = 33000.0 nM 4.48
CHEMBL3770860 IC50 = 33000.0 nM 4.48
CHEMBL3770553 IC50 = 45600.0 nM 4.34
CHEMBL3770486 IC50 = 65000.0 nM 4.19
CHEMBL3770474 IC50 = 77800.0 nM 4.11
CHEMBL3769476 IC50 = 127200.0 nM -
CHEMBL3771014 IC50 > 100000.0 nM -
CHEMBL3771167 IC50 = 289000.0 nM -
CHEMBL3769737 IC50 = 207000.0 nM -
CHEMBL3770074 IC50 = 143000.0 nM -
CHEMBL3770610 IC50 = 502800.0 nM -
CHEMBL3770257 IC50 = 167700.0 nM -
CHEMBL3771179 IC50 = 164500.0 nM -