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Assay Detail

CHEMBL3877360

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

Binding
Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay
1
Total Activities
1
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

Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
Yang EG, Mustafa N, Tan EC, Poulsen A, Ramanujulu PM, Chng WJ, Yen JJ, Dymock BW.
J Med Chem (2016) 59 : 8233 -8262
PubMed 27541357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.31 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3917405 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3917405 IC50 = 49.0 nM 7.31