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Assay Detail

CHEMBL4823336

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Binding
Inhibition of HDAC in human A2780 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 18 hrs followed by susbtrate addition and measured after 3 hrs by fluorescence microplate reader assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
Alves Avelar LA, Schrenk C, Sönnichsen M, Hamacher A, Hansen FK, Schliehe-Diecks J, Borkhardt A, Bhatia S, Kassack MU, Kurz T.
Eur J Med Chem (2021) 211 : 113095 -113095
PubMed 33360560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.95 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875953 1 6.72
CHEMBL4870868 1 6.60
CHEMBL4876405 1 6.46
CHEMBL4866536 1 6.32
CHEMBL4876613 1 6.22
CHEMBL4849008 1 6.19
CHEMBL4850081 1 6.17
CHEMBL4863947 1 6.15
CHEMBL4863503 1 6.13
CHEMBL4848096 1 6.07
CHEMBL4846633 1 5.87
CHEMBL4856574 1 5.80
CHEMBL98 VORINOSTAT 4.0 1 5.78
CHEMBL4872129 1 5.77
CHEMBL4874486 1 5.62
CHEMBL4856406 1 5.57
CHEMBL4866591 1 5.43
CHEMBL4878601 1 5.12
CHEMBL4873971 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875953 IC50 = 190.0 nM 6.72
CHEMBL4870868 IC50 = 250.0 nM 6.60
CHEMBL4876405 IC50 = 350.0 nM 6.46
CHEMBL4866536 IC50 = 480.0 nM 6.32
CHEMBL4876613 IC50 = 600.0 nM 6.22
CHEMBL4849008 IC50 = 640.0 nM 6.19
CHEMBL4850081 IC50 = 670.0 nM 6.17
CHEMBL4863947 IC50 = 710.0 nM 6.15
CHEMBL4863503 IC50 = 740.0 nM 6.13
CHEMBL4848096 IC50 = 850.0 nM 6.07
CHEMBL4846633 IC50 = 1360.0 nM 5.87
CHEMBL4856574 IC50 = 1580.0 nM 5.80
CHEMBL98 VORINOSTAT IC50 = 1680.0 nM 5.78
CHEMBL4872129 IC50 = 1710.0 nM 5.77
CHEMBL4874486 IC50 = 2390.0 nM 5.62
CHEMBL4856406 IC50 = 2700.0 nM 5.57
CHEMBL4866591 IC50 = 3710.0 nM 5.43
CHEMBL4878601 IC50 = 7680.0 nM 5.12
CHEMBL4873971 IC50 = 9080.0 nM 5.04