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Assay Detail

CHEMBL1838190

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

Binding
Inhibition of recombinant human HDAC4 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay
6
Total Activities
6
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 4 (CHEMBL3524)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
Wang C, Henkes LM, Doughty LB, He M, Wang D, Meyer-Almes FJ, Cheng YQ.
J Nat Prod (2011) 74 : 2031 -2038
PubMed 21793558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.03 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146250 FR-135313 -1.0 1 6.33
CHEMBL1836042 1 4.75
CHEMBL1836145 THAILANDEPSIN B 1 4.66
CHEMBL1836144 1 4.38
CHEMBL343448 ROMIDEPSIN 4.0 1 -
CHEMBL1836142 THAILANDEPSIN A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146250 FR-135313 IC50 = 470.0 nM 6.33
CHEMBL1836042 IC50 = 18000.0 nM 4.75
CHEMBL1836145 THAILANDEPSIN B IC50 = 22000.0 nM 4.66
CHEMBL1836144 IC50 = 42000.0 nM 4.38
CHEMBL343448 ROMIDEPSIN IC50 > 50000.0 nM -
CHEMBL1836142 THAILANDEPSIN A IC50 > 50000.0 nM -