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Assay Detail

CHEMBL4684792

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

Binding
Inhibition of human recombinant HDAC2 preincubated for 10 mins followed by addition of substrate fluor De Lys green measured after 30 mins by fluorescent plate reader analysis
3
Total Activities
3
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
Cheng C,Yun F,Ullah S,Yuan Q
Eur J Med Chem (2020) 189 : 112073 -112073
PubMed 31991336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.95 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745240 1 6.62
CHEMBL4761880 1 6.60
CHEMBL4087968 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745240 IC50 = 240.0 nM 6.62
CHEMBL4761880 IC50 = 250.0 nM 6.60
CHEMBL4087968 IC50 = 23000.0 nM 4.64