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Assay Detail

CHEMBL1838188

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

Binding
Inhibition of recombinant human HDAC2/NCOR2 using Boc-L-Lys(epsilon-acetyl)-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 7 — Homologous single protein target
Curated By Autocuration

Target

Histone deacetylase 2/Nuclear receptor corepressor 2 (CHEMBL3885591)
Type PROTEIN COMPLEX
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 6.77 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836144 1 8.46
CHEMBL146250 FR-135313 -1.0 1 8.41
CHEMBL1836042 1 8.17
CHEMBL343448 ROMIDEPSIN 4.0 1 5.82
CHEMBL1836145 THAILANDEPSIN B 1 5.35
CHEMBL1836142 THAILANDEPSIN A 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836144 IC50 = 3.5 nM 8.46
CHEMBL146250 FR-135313 IC50 = 3.9 nM 8.41
CHEMBL1836042 IC50 = 6.7 nM 8.17
CHEMBL343448 ROMIDEPSIN IC50 = 1500.0 nM 5.82
CHEMBL1836145 THAILANDEPSIN B IC50 = 4500.0 nM 5.35
CHEMBL1836142 THAILANDEPSIN A IC50 = 39000.0 nM 4.41