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Assay Detail

CHEMBL2188465

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

Binding
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.
Bergman JA, Woan K, Perez-Villarroel P, Villagra A, Sotomayor EM, Kozikowski AP.
J Med Chem (2012) 55 : 9891 -9899
PubMed 23009203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.84 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.30
CHEMBL272980 MOCETINOSTAT 2.0 1 6.99
CHEMBL2179247 1 6.58
CHEMBL2179246 1 5.87
CHEMBL2179245 1 5.87
CHEMBL2179615 1 5.77
CHEMBL2179249 1 5.72
CHEMBL2179617 1 5.65
CHEMBL2179248 1 5.59
CHEMBL2179618 NEXTURASTAT A 1 5.52
CHEMBL2179619 1 5.51
CHEMBL2179616 1 5.29
CHEMBL2179244 1 5.09
CHEMBL2179250 1 5.05
CHEMBL2018302 TUBASTATIN A 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 5.0 nM 8.30
CHEMBL272980 MOCETINOSTAT IC50 = 102.0 nM 6.99
CHEMBL2179247 IC50 = 265.0 nM 6.58
CHEMBL2179246 IC50 = 1360.0 nM 5.87
CHEMBL2179245 IC50 = 1360.0 nM 5.87
CHEMBL2179615 IC50 = 1690.0 nM 5.77
CHEMBL2179249 IC50 = 1910.0 nM 5.72
CHEMBL2179617 IC50 = 2250.0 nM 5.65
CHEMBL2179248 IC50 = 2550.0 nM 5.59
CHEMBL2179618 NEXTURASTAT A IC50 = 3020.0 nM 5.52
CHEMBL2179619 IC50 = 3120.0 nM 5.51
CHEMBL2179616 IC50 = 5180.0 nM 5.29
CHEMBL2179244 IC50 = 8120.0 nM 5.09
CHEMBL2179250 IC50 = 8950.0 nM 5.05
CHEMBL2018302 TUBASTATIN A IC50 = 16400.0 nM 4.79