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Assay Detail

CHEMBL873079

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Binding
Inhibition of in vitro enzyme activity measured in partially purified rat liver Histone deacetylase preparation
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2095943)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
Wittich S, Scherf H, Xie C, Brosch G, Loidl P, Gerhäuser C, Jung M.
J Med Chem (2002) 45 : 3296 -3309
PubMed 12109913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.37 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 7.92
CHEMBL331150 1 6.89
CHEMBL98 VORINOSTAT 4.0 1 6.78
CHEMBL320038 1 6.58
CHEMBL113003 1 6.54
CHEMBL111993 1 6.51
CHEMBL264629 1 6.50
CHEMBL326617 1 6.48
CHEMBL112652 1 6.42
CHEMBL111919 1 6.41
CHEMBL115271 1 6.39
CHEMBL113095 1 6.34
CHEMBL113337 1 6.29
CHEMBL46941 1 6.10
CHEMBL110906 1 6.10
CHEMBL323695 1 6.10
CHEMBL326022 1 6.08
CHEMBL109960 1 6.06
CHEMBL419029 1 6.00
CHEMBL320497 SUBEROHYDROXAMIC ACID 1 5.94
CHEMBL112728 1 5.87
CHEMBL325733 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 12.0 nM 7.92
CHEMBL331150 IC50 = 130.0 nM 6.89
CHEMBL98 VORINOSTAT IC50 = 165.0 nM 6.78
CHEMBL320038 IC50 = 260.0 nM 6.58
CHEMBL113003 IC50 = 290.0 nM 6.54
CHEMBL111993 IC50 = 310.0 nM 6.51
CHEMBL264629 IC50 = 320.0 nM 6.50
CHEMBL326617 IC50 = 330.0 nM 6.48
CHEMBL112652 IC50 = 380.0 nM 6.42
CHEMBL111919 IC50 = 390.0 nM 6.41
CHEMBL115271 IC50 = 410.0 nM 6.39
CHEMBL113095 IC50 = 460.0 nM 6.34
CHEMBL113337 IC50 = 510.0 nM 6.29
CHEMBL46941 IC50 = 800.0 nM 6.10
CHEMBL110906 IC50 = 790.0 nM 6.10
CHEMBL323695 IC50 = 800.0 nM 6.10
CHEMBL326022 IC50 = 840.0 nM 6.08
CHEMBL109960 IC50 = 880.0 nM 6.06
CHEMBL419029 IC50 = 1010.0 nM 6.00
CHEMBL320497 SUBEROHYDROXAMIC ACID IC50 = 1150.0 nM 5.94
CHEMBL112728 IC50 = 1340.0 nM 5.87
CHEMBL325733 IC50 = 1540.0 nM 5.81