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Assay Detail

CHEMBL4729565

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

Binding
Inhibition of HDAC1 (unknown origin)
5
Total Activities
5
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

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.
Noonepalle S,Shen S,Ptáček J,Tavares MT,Zhang G,Stránský J,Pavlíček J,Ferreira GM,Hadley M,Pelaez G,Bařinka C,Kozikowski AP,Villagra A
J Med Chem (2020) 63 : 10246 -10262
PubMed 32815366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.63 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935992 1 6.11
CHEMBL4783802 1 5.95
CHEMBL4469488 1 5.86
CHEMBL4761969 1 5.16
CHEMBL2018302 TUBASTATIN A 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935992 IC50 = 780.0 nM 6.11
CHEMBL4783802 IC50 = 1130.0 nM 5.95
CHEMBL4469488 IC50 = 1390.0 nM 5.86
CHEMBL4761969 IC50 = 6900.0 nM 5.16
CHEMBL2018302 TUBASTATIN A IC50 = 8100.0 nM 5.09