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Assay Detail

CHEMBL4625805

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

Binding
Inhibition of human recombinant HDAC8 expressed in Escherichia coli using FLUOR DE LYS as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence based assay
18
Total Activities
18
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 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Liu J, Kelly J, Yu W, Clausen D, Yu Y, Kim H, Duffy JL, Chung CC, Myers RW, Carroll S, Klein DJ, Fells J, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski JA.
ACS Med Chem Lett (2020) 11 : 1476 -1483
PubMed 32676157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.65 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4641682 1 8.52
CHEMBL4637689 1 7.80
CHEMBL4634501 1 7.50
CHEMBL4632775 1 7.00
CHEMBL4641904 1 6.67
CHEMBL4644307 1 6.55
CHEMBL4647458 1 6.42
CHEMBL4644721 1 6.35
CHEMBL4632449 1 6.33
CHEMBL4637836 1 6.22
CHEMBL4639586 1 5.30
CHEMBL4633968 1 5.10
CHEMBL4647164 1 -
CHEMBL4646763 1 -
CHEMBL4635130 1 -
CHEMBL4644575 1 -
CHEMBL4636534 1 -
CHEMBL4649382 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4641682 IC50 = 3.0 nM 8.52
CHEMBL4637689 IC50 = 16.0 nM 7.80
CHEMBL4634501 IC50 = 32.0 nM 7.50
CHEMBL4632775 IC50 = 100.0 nM 7.00
CHEMBL4641904 IC50 = 212.0 nM 6.67
CHEMBL4644307 IC50 = 280.0 nM 6.55
CHEMBL4647458 IC50 = 380.0 nM 6.42
CHEMBL4644721 IC50 = 445.0 nM 6.35
CHEMBL4632449 IC50 = 466.0 nM 6.33
CHEMBL4637836 IC50 = 603.0 nM 6.22
CHEMBL4639586 IC50 = 5000.0 nM 5.30
CHEMBL4633968 IC50 = 8000.0 nM 5.10
CHEMBL4647164 IC50 > 900.0 nM -
CHEMBL4646763 IC50 - -
CHEMBL4635130 IC50 - -
CHEMBL4644575 IC50 - -
CHEMBL4636534 IC50 > 1000.0 nM -
CHEMBL4649382 IC50 - -