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Assay Detail

CHEMBL1021292

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

Binding
Inhibition of recombinant HDAC1 by fluorimetric assay
ChEMBL ↗
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Histone deacetylase 1 (CHEMBL325) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
Wang H, Yu N, Song H, Chen D, Zou Y, Deng W, Lye PL, Chang J, Ng M, Sun ET, Sangthongpitag K, Wang X, Wu X, Khng HH, Fang L, Goh SK, Ong WC, Bonday Z, Stünkel W, Poulsen A, Entzeroth M.
Bioorg Med Chem Lett (2009) 19 : 1403 -1408
PubMed 19181524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.56 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489332 — — 1 7.58
CHEMBL491316 — — 1 7.46
CHEMBL460963 — — 1 7.39
CHEMBL491688 — — 1 7.33
CHEMBL491491 — — 1 7.28
CHEMBL474746 — — 1 7.10
CHEMBL475145 — — 1 7.00
CHEMBL98 VORINOSTAT 4.0 1 6.92
CHEMBL474349 — — 1 6.80
CHEMBL523601 — — 1 6.80
CHEMBL489125 — — 1 6.77
CHEMBL515906 — — 1 6.77
CHEMBL442585 — — 1 6.77
CHEMBL474152 — — 1 6.77
CHEMBL464719 — — 1 6.77
CHEMBL489331 — — 1 6.72
CHEMBL523646 — — 1 6.70
CHEMBL521909 — — 1 6.68
CHEMBL490721 — — 1 6.66
CHEMBL491490 — — 1 6.60
CHEMBL489706 — — 1 6.60
CHEMBL522269 — — 1 6.58
CHEMBL489709 — — 1 6.57
CHEMBL489330 — — 1 6.51
CHEMBL491687 — — 1 6.39
CHEMBL474151 — — 1 6.28
CHEMBL489124 — — 1 6.06
CHEMBL507008 — — 1 5.96
CHEMBL491282 — — 1 5.92
CHEMBL464927 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489332 — IC50 = 26.0 nM 7.58
CHEMBL491316 — IC50 = 35.0 nM 7.46
CHEMBL460963 — IC50 = 41.0 nM 7.39
CHEMBL491688 — IC50 = 47.0 nM 7.33
CHEMBL491491 — IC50 = 52.0 nM 7.28
CHEMBL474746 — IC50 = 80.0 nM 7.10
CHEMBL475145 — IC50 = 100.0 nM 7.00
CHEMBL98 VORINOSTAT IC50 = 120.0 nM 6.92
CHEMBL474349 — IC50 = 160.0 nM 6.80
CHEMBL523601 — IC50 = 160.0 nM 6.80
CHEMBL489125 — IC50 = 170.0 nM 6.77
CHEMBL464719 — IC50 = 170.0 nM 6.77
CHEMBL474152 — IC50 = 170.0 nM 6.77
CHEMBL442585 — IC50 = 170.0 nM 6.77
CHEMBL515906 — IC50 = 170.0 nM 6.77
CHEMBL489331 — IC50 = 190.0 nM 6.72
CHEMBL523646 — IC50 = 200.0 nM 6.70
CHEMBL521909 — IC50 = 210.0 nM 6.68
CHEMBL490721 — IC50 = 220.0 nM 6.66
CHEMBL489706 — IC50 = 250.0 nM 6.60
CHEMBL491490 — IC50 = 250.0 nM 6.60
CHEMBL522269 — IC50 = 260.0 nM 6.58
CHEMBL489709 — IC50 = 270.0 nM 6.57
CHEMBL489330 — IC50 = 310.0 nM 6.51
CHEMBL491687 — IC50 = 410.0 nM 6.39
CHEMBL474151 — IC50 = 530.0 nM 6.28
CHEMBL489124 — IC50 = 880.0 nM 6.06
CHEMBL507008 — IC50 = 1100.0 nM 5.96
CHEMBL491282 — IC50 = 1200.0 nM 5.92
CHEMBL464927 — IC50 = 1300.0 nM 5.89
CHEMBL474547 — IC50 = 1700.0 nM 5.77
CHEMBL474546 — IC50 = 1900.0 nM 5.72
CHEMBL490722 — IC50 = 2300.0 nM 5.64
CHEMBL474350 — IC50 = 3200.0 nM 5.50
CHEMBL464718 — IC50 = 3300.0 nM 5.48
CHEMBL461173 — IC50 > 10000.0 nM -
CHEMBL489902 — IC50 > 100000.0 nM -