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Assay Detail

CHEMBL4416947

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

Binding
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
64
Total Activities
64
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

Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation.
Vergani B, Sandrone G, Marchini M, Ripamonti C, Cellupica E, Galbiati E, Caprini G, Pavich G, Porro G, Rocchio I, Lattanzio M, Pezzuto M, Skorupska M, Cordella P, Pagani P, Pozzi P, Pomarico R, Modena D, Leoni F, Perego R, Fossati G, Steinkühler C, Stevenazzi A.
J Med Chem (2019) 62 : 10711 -10739
PubMed 31710483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 7.61 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4574641 1 9.00
CHEMBL4471726 1 8.70
CHEMBL3655950 1 8.70
CHEMBL4568509 1 8.52
CHEMBL4456695 1 8.52
CHEMBL4458053 1 8.52
CHEMBL4440425 1 8.40
CHEMBL4515782 1 8.40
CHEMBL4589682 1 8.40
CHEMBL4516856 1 8.30
CHEMBL4434656 1 8.30
CHEMBL4574536 1 8.30
CHEMBL4475365 1 8.30
CHEMBL4470373 1 8.30
CHEMBL4466468 1 8.22
CHEMBL4461219 1 8.22
CHEMBL4524728 1 8.22
CHEMBL4559109 1 8.22
CHEMBL4470302 1 8.22
CHEMBL4440341 1 8.15
CHEMBL4453121 1 8.15
CHEMBL4537736 1 8.10
CHEMBL4551987 1 8.05
CHEMBL4454663 1 8.05
CHEMBL4514075 1 8.05
CHEMBL4445138 1 8.05
CHEMBL4548513 1 8.00
CHEMBL4583522 1 8.00
CHEMBL4580311 1 7.96
CHEMBL2364628 RICOLINOSTAT 2.0 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4574641 IC50 = 1.0 nM 9.00
CHEMBL4471726 IC50 = 2.0 nM 8.70
CHEMBL3655950 IC50 = 2.0 nM 8.70
CHEMBL4568509 IC50 = 3.0 nM 8.52
CHEMBL4456695 IC50 = 3.0 nM 8.52
CHEMBL4458053 IC50 = 3.0 nM 8.52
CHEMBL4589682 IC50 = 4.0 nM 8.40
CHEMBL4515782 IC50 = 4.0 nM 8.40
CHEMBL4440425 IC50 = 4.0 nM 8.40
CHEMBL4475365 IC50 = 5.0 nM 8.30
CHEMBL4470373 IC50 = 5.0 nM 8.30
CHEMBL4574536 IC50 = 5.0 nM 8.30
CHEMBL4434656 IC50 = 5.0 nM 8.30
CHEMBL4516856 IC50 = 5.0 nM 8.30
CHEMBL4470302 IC50 = 6.0 nM 8.22
CHEMBL4466468 IC50 = 6.0 nM 8.22
CHEMBL4559109 IC50 = 6.0 nM 8.22
CHEMBL4524728 IC50 = 6.0 nM 8.22
CHEMBL4461219 IC50 = 6.0 nM 8.22
CHEMBL4440341 IC50 = 7.0 nM 8.15
CHEMBL4453121 IC50 = 7.0 nM 8.15
CHEMBL4537736 IC50 = 8.0 nM 8.10
CHEMBL4445138 IC50 = 9.0 nM 8.05
CHEMBL4514075 IC50 = 9.0 nM 8.05
CHEMBL4551987 IC50 = 9.0 nM 8.05
CHEMBL4454663 IC50 = 9.0 nM 8.05
CHEMBL4548513 IC50 = 10.0 nM 8.00
CHEMBL4583522 IC50 = 10.0 nM 8.00
CHEMBL4580311 IC50 = 11.0 nM 7.96
CHEMBL2364628 RICOLINOSTAT IC50 = 12.0 nM 7.92
CHEMBL4559028 IC50 = 12.0 nM 7.92
CHEMBL4556171 IC50 = 13.0 nM 7.89
CHEMBL4460868 IC50 = 16.0 nM 7.80
CHEMBL4438267 IC50 = 17.0 nM 7.77
CHEMBL4448410 IC50 = 17.0 nM 7.77
CHEMBL4535144 IC50 = 20.0 nM 7.70
CHEMBL4529251 IC50 = 20.0 nM 7.70
CHEMBL2018302 TUBASTATIN A IC50 = 21.0 nM 7.68
CHEMBL4439065 IC50 = 22.0 nM 7.66
CHEMBL2179618 NEXTURASTAT A IC50 = 25.0 nM 7.60
CHEMBL4551484 IC50 = 25.0 nM 7.60
CHEMBL4454925 IC50 = 25.0 nM 7.60
CHEMBL4515650 IC50 = 26.0 nM 7.58
CHEMBL1213492 GIVINOSTAT IC50 = 44.0 nM 7.36
CHEMBL4464235 IC50 = 52.0 nM 7.28
CHEMBL4545033 IC50 = 56.0 nM 7.25
CHEMBL4550551 IC50 = 62.0 nM 7.21
CHEMBL4436726 IC50 = 66.0 nM 7.18
CHEMBL3970950 IC50 = 102.0 nM 6.99
CHEMBL4066043 IC50 = 121.0 nM 6.92