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Assay Detail

CHEMBL4818541

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

Binding
Inhibition of recombinant human C-terminal FLAG-tagged HDAC1 expressed in human HEK293F cells using Fluor-de-lys substrate as substrate incubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence based assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Beshore DC, Adam GC, Barnard RJO, Burlein C, Gallicchio SN, Holloway MK, Krosky D, Lemaire W, Myers RW, Patel S, Plotkin MA, Powell DA, Rada V, Cox CD, Coleman PJ, Klein DJ, Wolkenberg SE.
ACS Med Chem Lett (2021) 12 : 540 -547
PubMed 33854701 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.70 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873847 1 9.00
CHEMBL2448576 1 8.70
CHEMBL4867665 1 8.70
CHEMBL4879154 1 7.80
CHEMBL4861270 1 7.43
CHEMBL4872186 1 7.33
CHEMBL4858081 1 6.60
CHEMBL4851511 1 6.55
CHEMBL4862719 1 6.41
CHEMBL4874919 1 6.11
CHEMBL4877454 1 5.33
CHEMBL4878011 1 4.75
CHEMBL4859130 1 4.64
CHEMBL4855240 1 4.39
CHEMBL4851062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873847 IC50 = 1.0 nM 9.00
CHEMBL2448576 IC50 = 2.0 nM 8.70
CHEMBL4867665 IC50 = 2.0 nM 8.70
CHEMBL4879154 IC50 = 16.0 nM 7.80
CHEMBL4861270 IC50 = 37.0 nM 7.43
CHEMBL4872186 IC50 = 47.0 nM 7.33
CHEMBL4858081 IC50 = 250.0 nM 6.60
CHEMBL4851511 IC50 = 280.0 nM 6.55
CHEMBL4862719 IC50 = 390.0 nM 6.41
CHEMBL4874919 IC50 = 770.0 nM 6.11
CHEMBL4877454 IC50 = 4700.0 nM 5.33
CHEMBL4878011 IC50 = 18000.0 nM 4.75
CHEMBL4859130 IC50 = 23000.0 nM 4.64
CHEMBL4855240 IC50 = 41000.0 nM 4.39
CHEMBL4851062 IC50 > 50000.0 nM -