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Assay Detail

CHEMBL4355679

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

Binding
Inhibition of recombinant human HDAC1 expressed in HEK293T/17 cells using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay
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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
Shen S, Hadley M, Ustinova K, Pavlicek J, Knox T, Noonepalle S, Tavares MT, Zimprich CA, Zhang G, Robers MB, Bařinka C, Kozikowski AP, Villagra A.
J Med Chem (2019) 62 : 8557 -8577
PubMed 31414801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.59 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447715 1 7.47
CHEMBL2179618 NEXTURASTAT A 1 6.44
CHEMBL4469488 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447715 IC50 = 34.0 nM 7.47
CHEMBL2179618 NEXTURASTAT A IC50 = 360.0 nM 6.44
CHEMBL4469488 IC50 = 1390.0 nM 5.86