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Assay Detail

CHEMBL693167

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

Binding
Inhibitory activity against mixture of histone deacetylase 1 (HDAC1) and histone deacetylase 2 (HDAC2) from nuclear extraction of K562 erythroleukemia cells.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Histone deacetylase (HDAC1 and HDAC2) (CHEMBL2111429)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Alpha-keto amides as inhibitors of histone deacetylase.
Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2003) 13 : 3331 -3335
PubMed 12951120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 8.05 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114184 1 10.70
CHEMBL432618 1 10.21
CHEMBL321689 1 10.09
CHEMBL432243 1 9.96
CHEMBL113303 1 9.96
CHEMBL112984 1 8.85
CHEMBL113033 1 8.51
CHEMBL112446 1 8.43
CHEMBL115049 1 8.43
CHEMBL113034 1 8.37
CHEMBL321253 1 8.31
CHEMBL324429 1 8.04
CHEMBL420300 1 8.03
CHEMBL111898 1 8.02
CHEMBL333150 1 7.96
CHEMBL113094 1 7.75
CHEMBL320921 1 7.68
CHEMBL112340 1 6.88
CHEMBL112742 1 6.84
CHEMBL444534 1 6.70
CHEMBL113093 1 6.62
CHEMBL112211 1 6.47
CHEMBL113156 1 6.28
CHEMBL112171 1 6.07
CHEMBL322710 1 5.98
CHEMBL326842 1 -
CHEMBL325736 1 -
CHEMBL113566 1 -
CHEMBL113495 1 -
CHEMBL265564 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114184 IC50 = 0.02 nM 10.70
CHEMBL432618 IC50 = 0.062 nM 10.21
CHEMBL321689 IC50 = 0.082 nM 10.09
CHEMBL432243 IC50 = 0.109 nM 9.96
CHEMBL113303 IC50 = 0.11 nM 9.96
CHEMBL112984 IC50 = 1.4 nM 8.85
CHEMBL113033 IC50 = 3.1 nM 8.51
CHEMBL112446 IC50 = 3.7 nM 8.43
CHEMBL115049 IC50 = 3.7 nM 8.43
CHEMBL113034 IC50 = 4.3 nM 8.37
CHEMBL321253 IC50 = 4.9 nM 8.31
CHEMBL324429 IC50 = 9.1 nM 8.04
CHEMBL420300 IC50 = 9.4 nM 8.03
CHEMBL111898 IC50 = 9.5 nM 8.02
CHEMBL333150 IC50 = 11.0 nM 7.96
CHEMBL113094 IC50 = 18.0 nM 7.75
CHEMBL320921 IC50 = 21.0 nM 7.68
CHEMBL112340 IC50 = 133.0 nM 6.88
CHEMBL112742 IC50 = 143.0 nM 6.84
CHEMBL444534 IC50 = 201.0 nM 6.70
CHEMBL113093 IC50 = 241.0 nM 6.62
CHEMBL112211 IC50 = 338.0 nM 6.47
CHEMBL113156 IC50 = 526.0 nM 6.28
CHEMBL112171 IC50 = 853.0 nM 6.07
CHEMBL322710 IC50 = 1041.0 nM 5.98
CHEMBL326842 IC50 > 1000.0 nM -
CHEMBL325736 IC50 > 10000.0 nM -
CHEMBL113566 IC50 > 5.0 nM -
CHEMBL113495 IC50 > 50.0 nM -
CHEMBL265564 IC50 > 50.0 nM -
CHEMBL113367 IC50 > 50.0 nM -
CHEMBL112148 IC50 = 2.9 nM -