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Assay Detail

CHEMBL5638243

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

Binding
Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hrs followed by substrate addition and measured after 2 hrs by spectrophotometer based fluorometric assay
21
Total Activities
21
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells.
Deng J, Hou B, Hou X, Chen Y, Zhang T, Chen H, Wang Y, Li X.
Eur J Med Chem (2023) 262 : 115915 -115915
PubMed 37948955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.51 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5639904 1 6.89
CHEMBL5647223 1 6.77
CHEMBL5639636 1 6.62
CHEMBL5639136 1 6.61
CHEMBL5646494 1 6.53
CHEMBL235191 TACEDINALINE 3.0 1 6.44
CHEMBL5639135 1 6.35
CHEMBL5641600 1 6.34
CHEMBL5639599 1 6.31
CHEMBL5641748 1 6.22
CHEMBL5639202 1 -
CHEMBL5639918 1 -
CHEMBL5646792 1 -
CHEMBL5639397 1 -
CHEMBL5647361 1 -
CHEMBL5646831 1 -
CHEMBL5639116 1 -
CHEMBL5639808 1 -
CHEMBL5647285 1 -
CHEMBL5639572 1 -
CHEMBL5646723 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5639904 IC50 = 127.8 nM 6.89
CHEMBL5647223 IC50 = 168.2 nM 6.77
CHEMBL5639636 IC50 = 240.7 nM 6.62
CHEMBL5639136 IC50 = 247.2 nM 6.61
CHEMBL5646494 IC50 = 295.3 nM 6.53
CHEMBL235191 TACEDINALINE IC50 = 363.9 nM 6.44
CHEMBL5639135 IC50 = 443.3 nM 6.35
CHEMBL5641600 IC50 = 459.1 nM 6.34
CHEMBL5639599 IC50 = 489.8 nM 6.31
CHEMBL5641748 IC50 = 602.2 nM 6.22
CHEMBL5639202 IC50 > 10000.0 nM -
CHEMBL5639918 IC50 > 10000.0 nM -
CHEMBL5646792 IC50 > 10000.0 nM -
CHEMBL5639397 IC50 > 10000.0 nM -
CHEMBL5647361 IC50 > 10000.0 nM -
CHEMBL5646831 IC50 > 10000.0 nM -
CHEMBL5639116 IC50 > 10000.0 nM -
CHEMBL5639808 IC50 > 10000.0 nM -
CHEMBL5647285 IC50 > 10000.0 nM -
CHEMBL5639572 IC50 > 10000.0 nM -
CHEMBL5646723 IC50 > 10000.0 nM -