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Assay Detail

CHEMBL3112170

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

Binding
Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay
14
Total Activities
14
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 3 (CHEMBL1829)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
Bürli RW, Luckhurst CA, Aziz O, Matthews KL, Yates D, Lyons KA, Beconi M, McAllister G, Breccia P, Stott AJ, Penrose SD, Wall M, Lamers M, Leonard P, Müller I, Richardson CM, Jarvis R, Stones L, Hughes S, Wishart G, Haughan AF, O'Connell C, Mead T, McNeil H, Vann J, Mangette J, Maillard M, Beaumont V, Munoz-Sanjuan I, Dominguez C.
J Med Chem (2013) 56 : 9934 -9954
PubMed 24261862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.08 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 6.60
CHEMBL518821 1 6.42
CHEMBL3109980 1 5.33
CHEMBL3110001 1 5.05
CHEMBL3110015 1 5.03
CHEMBL3110021 1 4.92
CHEMBL3109983 1 4.80
CHEMBL3109993 1 4.75
CHEMBL3110023 1 4.60
CHEMBL3110016 1 4.58
CHEMBL3110005 1 4.48
CHEMBL3110003 1 4.41
CHEMBL3110004 1 -
CHEMBL396097 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 250.0 nM 6.60
CHEMBL518821 IC50 = 380.0 nM 6.42
CHEMBL3109980 IC50 = 4700.0 nM 5.33
CHEMBL3110001 IC50 = 8900.0 nM 5.05
CHEMBL3110015 IC50 = 9400.0 nM 5.03
CHEMBL3110021 IC50 = 12000.0 nM 4.92
CHEMBL3109983 IC50 = 16000.0 nM 4.80
CHEMBL3109993 IC50 = 18000.0 nM 4.75
CHEMBL3110023 IC50 = 25000.0 nM 4.60
CHEMBL3110016 IC50 = 26000.0 nM 4.58
CHEMBL3110005 IC50 = 33000.0 nM 4.48
CHEMBL3110003 IC50 = 39000.0 nM 4.41
CHEMBL3110004 IC50 > 43000.0 nM -
CHEMBL396097 IC50 > 50000.0 nM -