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Assay Detail

CHEMBL5332398

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

Binding
Inhibition of human HDAC1 using Boc-Lys (acetyl)-AMC as substrate pretreated with compound for 1 hrs followed by substrate addition measured after 1 hrs by microplate reader analysis
ChEMBL ↗
46
Total Activities
46
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 1 (CHEMBL325) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and anticancer activity of novel histone deacetylase inhibitors that inhibit autophagy and induce apoptosis.
Mo H, Zhang R, Chen Y, Li S, Wang Y, Zou W, Lin Q, Zhao DG, Du Y, Zhang K, Ma YY.
Eur J Med Chem (2022) 243 : 114705 -114705
PubMed 36215854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.02 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399106 — — 1 7.70
CHEMBL5410523 — — 1 7.53
CHEMBL5402344 — — 1 7.50
CHEMBL5418695 — — 1 7.49
CHEMBL5434626 — — 1 7.48
CHEMBL5416448 — — 1 7.44
CHEMBL5418936 — — 1 7.40
CHEMBL5424823 — — 1 7.37
CHEMBL5406583 — — 1 7.35
CHEMBL5440176 — — 1 7.27
CHEMBL5420954 — — 1 7.23
CHEMBL5414056 — — 1 7.22
CHEMBL5394600 — — 1 7.22
CHEMBL5410992 — — 1 7.19
CHEMBL5438694 — — 1 7.18
CHEMBL5432886 — — 1 7.18
CHEMBL5412747 — — 1 7.18
CHEMBL5413000 — — 1 7.18
CHEMBL5431676 — — 1 7.17
CHEMBL5422333 — — 1 7.14
CHEMBL5417760 — — 1 7.09
CHEMBL5436704 — — 1 7.07
CHEMBL5395752 — — 1 7.02
CHEMBL5408565 — — 1 6.99
CHEMBL98 VORINOSTAT 4.0 1 6.97
CHEMBL5435909 — — 1 6.94
CHEMBL5440733 — — 1 6.91
CHEMBL5436596 — — 1 6.85
CHEMBL5409321 — — 1 6.76
CHEMBL5409830 — — 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399106 — IC50 = 19.75 nM 7.70
CHEMBL5410523 — IC50 = 29.5 nM 7.53
CHEMBL5402344 — IC50 = 31.38 nM 7.50
CHEMBL5418695 — IC50 = 32.73 nM 7.49
CHEMBL5434626 — IC50 = 32.97 nM 7.48
CHEMBL5416448 — IC50 = 36.42 nM 7.44
CHEMBL5418936 — IC50 = 40.07 nM 7.40
CHEMBL5424823 — IC50 = 42.82 nM 7.37
CHEMBL5406583 — IC50 = 44.41 nM 7.35
CHEMBL5440176 — IC50 = 53.62 nM 7.27
CHEMBL5420954 — IC50 = 59.34 nM 7.23
CHEMBL5414056 — IC50 = 60.24 nM 7.22
CHEMBL5394600 — IC50 = 60.31 nM 7.22
CHEMBL5410992 — IC50 = 63.91 nM 7.19
CHEMBL5413000 — IC50 = 65.7 nM 7.18
CHEMBL5438694 — IC50 = 65.27 nM 7.18
CHEMBL5412747 — IC50 = 66.72 nM 7.18
CHEMBL5432886 — IC50 = 66.34 nM 7.18
CHEMBL5431676 — IC50 = 67.79 nM 7.17
CHEMBL5422333 — IC50 = 72.3 nM 7.14
CHEMBL5417760 — IC50 = 81.2 nM 7.09
CHEMBL5436704 — IC50 = 84.64 nM 7.07
CHEMBL5395752 — IC50 = 95.67 nM 7.02
CHEMBL5408565 — IC50 = 102.7 nM 6.99
CHEMBL98 VORINOSTAT IC50 = 106.13 nM 6.97
CHEMBL5435909 — IC50 = 115.3 nM 6.94
CHEMBL5440733 — IC50 = 124.25 nM 6.91
CHEMBL5436596 — IC50 = 141.55 nM 6.85
CHEMBL5409321 — IC50 = 172.4 nM 6.76
CHEMBL5409830 — IC50 = 181.2 nM 6.74
CHEMBL5420058 — IC50 = 197.1 nM 6.71
CHEMBL5426471 — IC50 = 193.6 nM 6.71
CHEMBL5423136 — IC50 = 215.2 nM 6.67
CHEMBL5410777 — IC50 = 247.5 nM 6.61
CHEMBL5403601 — IC50 = 282.6 nM 6.55
CHEMBL5395429 — IC50 = 310.5 nM 6.51
CHEMBL5432519 — IC50 = 305.2 nM 6.51
CHEMBL5410667 — IC50 = 312.4 nM 6.50
CHEMBL5431600 — IC50 = 407.6 nM 6.39
CHEMBL5402253 — IC50 = 937.2 nM 6.03
CHEMBL5407960 — IC50 > 1000.0 nM -
CHEMBL5433541 — IC50 > 1000.0 nM -
CHEMBL5401609 — IC50 > 1000.0 nM -
CHEMBL5432005 — IC50 > 1000.0 nM -
CHEMBL5429362 — IC50 > 1000.0 nM -
CHEMBL5427531 — IC50 > 1000.0 nM -