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Assay Detail

CHEMBL940370

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

Binding
Inhibition of human HDAC2 expressed in mammalian cells
8
Total Activities
8
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

SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA.
Bioorg Med Chem Lett (2008) 18 : 6104 -6109
PubMed 18951790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.54 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513568 1 7.36
CHEMBL511797 1 7.15
CHEMBL471824 1 6.96
CHEMBL269935 1 6.70
CHEMBL236902 1 6.51
CHEMBL256440 1 6.41
CHEMBL255805 1 6.05
CHEMBL236678 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513568 IC50 = 44.0 nM 7.36
CHEMBL511797 IC50 = 71.0 nM 7.15
CHEMBL471824 IC50 = 110.0 nM 6.96
CHEMBL269935 IC50 = 200.0 nM 6.70
CHEMBL236902 IC50 = 308.0 nM 6.51
CHEMBL256440 IC50 = 390.0 nM 6.41
CHEMBL255805 IC50 = 900.0 nM 6.05
CHEMBL236678 IC50 = 6980.0 nM 5.16