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Assay Detail

CHEMBL4830944

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

Binding
Inhibition of human recombinant SIRT5 (34 to 269 residues) using Ac-Leu-Gly-Ser-Lys(Su)-AMC as substrate in presence of NAD+ by fluorescence based analysis
ChEMBL ↗
93
Total Activities
48
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 deacylase sirtuin-5, mitochondrial (CHEMBL2163183) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new human Sirtuin 5 inhibitors by mimicking glutaryl-lysine substrates.
Yang F, Su H, Deng J, Mou L, Wang H, Li R, Dai QQ, Yan YH, Qian S, Wang Z, Li GB, Yang L.
Eur J Med Chem (2021) 225 : 113803 -113803
PubMed 34461505 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 93 4.67 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875043 — — 2 5.52
CHEMBL4860183 — — 2 5.48
CHEMBL4869330 — — 2 5.36
CHEMBL4859582 — — 2 5.16
CHEMBL4859500 — — 2 5.16
CHEMBL4868469 — — 2 5.04
CHEMBL4848386 — — 2 5.03
CHEMBL4879062 — — 2 5.02
CHEMBL4849909 — — 2 5.02
CHEMBL4872703 — — 2 4.90
CHEMBL4853872 — — 2 4.86
CHEMBL4866019 — — 2 4.85
CHEMBL4866354 — — 2 4.81
CHEMBL4849090 — — 2 4.81
CHEMBL4858067 — — 2 4.79
CHEMBL4871368 — — 2 4.68
CHEMBL4861845 — — 2 4.66
CHEMBL4849282 — — 2 4.64
CHEMBL265502 SURAMIN 3.0 2 4.64
CHEMBL4877152 — — 2 4.57
CHEMBL4849964 — — 2 4.54
CHEMBL4870297 — — 2 4.54
CHEMBL4852253 — — 2 4.52
CHEMBL4859872 — — 2 4.52
CHEMBL4877318 — — 2 4.50
CHEMBL4865077 — — 2 4.49
CHEMBL4877652 — — 2 4.47
CHEMBL4869704 — — 2 4.46
CHEMBL4862462 — — 2 4.43
CHEMBL4854363 — — 2 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875043 — IC50 = 3000.0 nM 5.52
CHEMBL4875043 — IC50 = 3076.1 nM 5.51
CHEMBL4860183 — IC50 = 3300.0 nM 5.48
CHEMBL4860183 — IC50 = 3341.95 nM 5.48
CHEMBL4869330 — IC50 = 4400.0 nM 5.36
CHEMBL4869330 — IC50 = 4436.09 nM 5.35
CHEMBL4859582 — IC50 = 6982.32 nM 5.16
CHEMBL4859582 — IC50 = 6900.0 nM 5.16
CHEMBL4859500 — IC50 = 6900.0 nM 5.16
CHEMBL4859500 — IC50 = 6966.27 nM 5.16
CHEMBL4868469 — IC50 = 9141.13 nM 5.04
CHEMBL4868469 — IC50 = 9100.0 nM 5.04
CHEMBL4848386 — IC50 = 9375.62 nM 5.03
CHEMBL4848386 — IC50 = 9400.0 nM 5.03
CHEMBL4879062 — IC50 = 9600.0 nM 5.02
CHEMBL4849909 — IC50 = 9600.0 nM 5.02
CHEMBL4879062 — IC50 = 9594.01 nM 5.02
CHEMBL4849909 — IC50 = 9660.51 nM 5.01
CHEMBL4872703 — IC50 = 12700.0 nM 4.90
CHEMBL4872703 — IC50 = 12735.03 nM 4.89
CHEMBL4853872 — IC50 = 13867.56 nM 4.86
CHEMBL4853872 — IC50 = 13900.0 nM 4.86
CHEMBL4866019 — IC50 = 14190.58 nM 4.85
CHEMBL4866019 — IC50 = 14200.0 nM 4.85
CHEMBL4849090 — IC50 = 15600.0 nM 4.81
CHEMBL4866354 — IC50 = 15417.0 nM 4.81
CHEMBL4866354 — IC50 = 15400.0 nM 4.81
CHEMBL4849090 — IC50 = 15559.66 nM 4.81
CHEMBL4858067 — IC50 = 16255.49 nM 4.79
CHEMBL4858067 — IC50 = 16230.0 nM 4.79
CHEMBL4871368 — IC50 = 20892.96 nM 4.68
CHEMBL4871368 — IC50 = 20900.0 nM 4.68
CHEMBL4861845 — IC50 = 22100.0 nM 4.66
CHEMBL4849282 — IC50 = 22800.0 nM 4.64
CHEMBL4849282 — IC50 = 22803.42 nM 4.64
CHEMBL265502 SURAMIN IC50 = 23120.65 nM 4.64
CHEMBL265502 SURAMIN IC50 = 23100.0 nM 4.64
CHEMBL4877152 — IC50 = 26668.59 nM 4.57
CHEMBL4877152 — IC50 = 26700.0 nM 4.57
CHEMBL4870297 — IC50 = 28800.0 nM 4.54
CHEMBL4849964 — IC50 = 28600.0 nM 4.54
CHEMBL4870297 — IC50 = 28773.98 nM 4.54
CHEMBL4849964 — IC50 = 28575.91 nM 4.54
CHEMBL4852253 — IC50 = 29922.65 nM 4.52
CHEMBL4859872 — IC50 = 30408.85 nM 4.52
CHEMBL4859872 — IC50 = 30400.0 nM 4.52
CHEMBL4852253 — IC50 = 29900.0 nM 4.52
CHEMBL4877318 — IC50 = 32000.0 nM 4.50
CHEMBL4865077 — IC50 = 32100.0 nM 4.49
CHEMBL4865077 — IC50 = 32136.61 nM 4.49