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Assay Detail

CHEMBL1034714

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

Binding
Inhibition of HDAC2 in human HeLa cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
Dallavalle S, Cincinelli R, Nannei R, Merlini L, Morini G, Penco S, Pisano C, Vesci L, Barbarino M, Zuco V, De Cesare M, Zunino F.
Eur J Med Chem (2009) 44 : 1900 -1912
PubMed 19084294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.24 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.00
CHEMBL551486 1 6.66
CHEMBL539156 1 6.51
CHEMBL555906 1 6.50
CHEMBL538710 1 6.48
CHEMBL561212 1 6.35
CHEMBL565140 1 6.34
CHEMBL556332 1 6.23
CHEMBL541239 1 6.14
CHEMBL556532 1 6.09
CHEMBL561209 1 5.94
CHEMBL538713 1 5.92
CHEMBL552750 1 5.92
CHEMBL551151 1 5.77
CHEMBL557066 1 5.73
CHEMBL554573 1 -
CHEMBL538712 1 -
CHEMBL538967 1 -
CHEMBL538364 1 -
CHEMBL562757 1 -
CHEMBL561411 1 -
CHEMBL551549 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 100.0 nM 7.00
CHEMBL551486 IC50 = 220.0 nM 6.66
CHEMBL539156 IC50 = 310.0 nM 6.51
CHEMBL555906 IC50 = 320.0 nM 6.50
CHEMBL538710 IC50 = 330.0 nM 6.48
CHEMBL561212 IC50 = 450.0 nM 6.35
CHEMBL565140 IC50 = 460.0 nM 6.34
CHEMBL556332 IC50 = 590.0 nM 6.23
CHEMBL541239 IC50 = 720.0 nM 6.14
CHEMBL556532 IC50 = 820.0 nM 6.09
CHEMBL561209 IC50 = 1160.0 nM 5.94
CHEMBL538713 IC50 = 1200.0 nM 5.92
CHEMBL552750 IC50 = 1200.0 nM 5.92
CHEMBL551151 IC50 = 1700.0 nM 5.77
CHEMBL557066 IC50 = 1860.0 nM 5.73
CHEMBL554573 IC50 > 5000.0 nM -
CHEMBL538712 IC50 > 5000.0 nM -
CHEMBL538967 IC50 > 5000.0 nM -
CHEMBL538364 IC50 > 5000.0 nM -
CHEMBL562757 IC50 - -
CHEMBL561411 IC50 - -
CHEMBL551549 IC50 - -