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Assay Detail

CHEMBL3598913

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

Binding
Inhibition of human HDAC2
10
Total Activities
10
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
Carrillo AK, Guiguemde WA, Guy RK.
Bioorg Med Chem (2015) 23 : 5151 -5155
PubMed 25637120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.62 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105763 QUISINOSTAT 2.0 1 10.22
CHEMBL314389 OXAMFLATIN 1 10.00
CHEMBL99 TRICHOSTATIN 1.0 1 9.15
CHEMBL483254 PANOBINOSTAT 4.0 1 9.15
CHEMBL408513 BELINOSTAT 4.0 1 9.05
CHEMBL356066 DACINOSTAT 2.0 1 8.85
CHEMBL1213492 GIVINOSTAT 4.0 1 8.52
CHEMBL2103863 ABEXINOSTAT 3.0 1 7.72
CHEMBL1851943 PRACINOSTAT 3.0 1 7.57
CHEMBL356769 TUBACIN 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105763 QUISINOSTAT Ki = 0.06 nM 10.22
CHEMBL314389 OXAMFLATIN Ki = 0.1 nM 10.00
CHEMBL99 TRICHOSTATIN Ki = 0.7 nM 9.15
CHEMBL483254 PANOBINOSTAT Ki = 0.7 nM 9.15
CHEMBL408513 BELINOSTAT Ki = 0.9 nM 9.05
CHEMBL356066 DACINOSTAT Ki = 1.4 nM 8.85
CHEMBL1213492 GIVINOSTAT Ki = 3.0 nM 8.52
CHEMBL2103863 ABEXINOSTAT Ki = 19.0 nM 7.72
CHEMBL1851943 PRACINOSTAT Ki = 27.0 nM 7.57
CHEMBL356769 TUBACIN Ki = 1180.7 nM 5.93