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Assay Detail

CHEMBL4198899

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

Binding
Inhibition of HDAC6 (unknown origin)
7
Total Activities
7
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

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

Publication

Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J.
Eur J Med Chem (2018) 150 : 506 -524
PubMed 29549837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.44 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356769 TUBACIN 1 8.40
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.33
CHEMBL2018302 TUBASTATIN A 1 7.82
CHEMBL98 VORINOSTAT 4.0 1 7.42
CHEMBL4066043 1 7.25
CHEMBL4208487 1 6.96
CHEMBL99 TRICHOSTATIN 1.0 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356769 TUBACIN IC50 = 4.0 nM 8.40
CHEMBL2364628 RICOLINOSTAT IC50 = 4.7 nM 8.33
CHEMBL2018302 TUBASTATIN A IC50 = 15.0 nM 7.82
CHEMBL98 VORINOSTAT IC50 = 38.0 nM 7.42
CHEMBL4066043 IC50 = 56.0 nM 7.25
CHEMBL4208487 IC50 = 110.0 nM 6.96
CHEMBL99 TRICHOSTATIN IC50 = 1210.0 nM 5.92