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Assay Detail

CHEMBL3238609

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Binding
Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate
8
Total Activities
8
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

Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
Cincinelli R, Musso L, Giannini G, Zuco V, De Cesare M, Zunino F, Dallavalle S.
Eur J Med Chem (2014) 79 : 251 -259
PubMed 24742384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.74 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 9.38
CHEMBL98 VORINOSTAT 4.0 1 7.54
CHEMBL561209 1 7.43
CHEMBL556332 1 7.38
CHEMBL3235790 1 6.39
CHEMBL3235463 1 5.55
CHEMBL538364 1 5.49
CHEMBL3235787 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 0.419 nM 9.38
CHEMBL98 VORINOSTAT IC50 = 28.6 nM 7.54
CHEMBL561209 IC50 = 36.8 nM 7.43
CHEMBL556332 IC50 = 41.8 nM 7.38
CHEMBL3235790 IC50 = 408.0 nM 6.39
CHEMBL3235463 IC50 = 2800.0 nM 5.55
CHEMBL538364 IC50 = 3260.0 nM 5.49
CHEMBL3235787 IC50 = 16700.0 nM 4.78