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Assay Detail

CHEMBL4708169

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

Binding
Inhibition of recombinant full length human HDAC6 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.
Gawel JM,Shouksmith AE,Raouf YS,Nawar N,Toutah K,Bukhari S,Manaswiyoungkul P,Olaoye OO,Israelian J,Radu TB,Cabral AD,Sina D,Sedighi A,de Araujo ED,Gunning PT
Eur J Med Chem (2020) 201 : 112411 -112411
PubMed 32615502 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.95 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4750701 1 8.84
CHEMBL4757957 1 8.80
CHEMBL4798826 1 8.70
CHEMBL3693786 CITARINOSTAT 2.0 1 8.66
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.59
CHEMBL4747455 1 8.55
CHEMBL4784006 1 8.23
CHEMBL4760306 1 8.17
CHEMBL4742241 1 7.98
CHEMBL4785378 1 7.92
CHEMBL4755724 1 7.89
CHEMBL4765007 1 7.85
CHEMBL4763401 1 7.85
CHEMBL4760053 1 7.76
CHEMBL4744157 1 7.76
CHEMBL4761127 1 7.74
CHEMBL4755326 1 7.68
CHEMBL4780745 1 7.65
CHEMBL4452620 1 7.61
CHEMBL4790223 1 7.58
CHEMBL4799423 1 7.49
CHEMBL4758855 1 7.38
CHEMBL4638377 1 7.15
CHEMBL4788731 1 7.01
CHEMBL4792001 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4750701 IC50 = 1.46 nM 8.84
CHEMBL4757957 IC50 = 1.6 nM 8.80
CHEMBL4798826 IC50 = 2.01 nM 8.70
CHEMBL3693786 CITARINOSTAT IC50 = 2.21 nM 8.66
CHEMBL2364628 RICOLINOSTAT IC50 = 2.59 nM 8.59
CHEMBL4747455 IC50 = 2.81 nM 8.55
CHEMBL4784006 IC50 = 5.92 nM 8.23
CHEMBL4760306 IC50 = 6.77 nM 8.17
CHEMBL4742241 IC50 = 10.4 nM 7.98
CHEMBL4785378 IC50 = 12.0 nM 7.92
CHEMBL4755724 IC50 = 13.0 nM 7.89
CHEMBL4765007 IC50 = 14.0 nM 7.85
CHEMBL4763401 IC50 = 14.0 nM 7.85
CHEMBL4760053 IC50 = 17.5 nM 7.76
CHEMBL4744157 IC50 = 17.3 nM 7.76
CHEMBL4761127 IC50 = 18.4 nM 7.74
CHEMBL4755326 IC50 = 20.9 nM 7.68
CHEMBL4780745 IC50 = 22.6 nM 7.65
CHEMBL4452620 IC50 = 24.4 nM 7.61
CHEMBL4790223 IC50 = 26.6 nM 7.58
CHEMBL4799423 IC50 = 32.4 nM 7.49
CHEMBL4758855 IC50 = 41.9 nM 7.38
CHEMBL4638377 IC50 = 71.1 nM 7.15
CHEMBL4788731 IC50 = 96.6 nM 7.01
CHEMBL4792001 IC50 > 1000.0 nM -