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Assay Detail

CHEMBL3112174

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

Binding
Inhibition of human recombinant HDAC4 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay
ChEMBL ↗
52
Total Activities
52
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 4 (CHEMBL3524) ↗
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 52 6.85 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3109999 — — 1 8.00
CHEMBL518821 — — 1 8.00
CHEMBL3110021 — — 1 7.70
CHEMBL3109993 — — 1 7.70
CHEMBL3109980 — — 1 7.70
CHEMBL3109977 — — 1 7.70
CHEMBL3110001 — — 1 7.70
CHEMBL3109984 — — 1 7.52
CHEMBL3109983 — — 1 7.52
CHEMBL3109979 — — 1 7.52
CHEMBL3109978 — — 1 7.52
CHEMBL3109985 — — 1 7.40
CHEMBL3109982 — — 1 7.40
CHEMBL3109987 — — 1 7.40
CHEMBL3110000 — — 1 7.40
CHEMBL3109981 — — 1 7.40
CHEMBL3110015 — — 1 7.30
CHEMBL3110020 — — 1 7.30
CHEMBL3110014 — — 1 7.22
CHEMBL3110019 — — 1 7.22
CHEMBL3109986 — — 1 7.22
CHEMBL3110002 — — 1 7.10
CHEMBL3110012 — — 1 7.10
CHEMBL3109988 — — 1 7.00
CHEMBL3110013 — — 1 7.00
CHEMBL3110016 — — 1 7.00
CHEMBL3110018 — — 1 7.00
CHEMBL3110004 — — 1 6.89
CHEMBL3110010 — — 1 6.82
CHEMBL3110011 — — 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3109999 — IC50 = 10.0 nM 8.00
CHEMBL518821 — IC50 = 10.0 nM 8.00
CHEMBL3109993 — IC50 = 20.0 nM 7.70
CHEMBL3109980 — IC50 = 20.0 nM 7.70
CHEMBL3109977 — IC50 = 20.0 nM 7.70
CHEMBL3110001 — IC50 = 20.0 nM 7.70
CHEMBL3110021 — IC50 = 20.0 nM 7.70
CHEMBL3109984 — IC50 = 30.0 nM 7.52
CHEMBL3109983 — IC50 = 30.0 nM 7.52
CHEMBL3109979 — IC50 = 30.0 nM 7.52
CHEMBL3109978 — IC50 = 30.0 nM 7.52
CHEMBL3109981 — IC50 = 40.0 nM 7.40
CHEMBL3109985 — IC50 = 40.0 nM 7.40
CHEMBL3109982 — IC50 = 40.0 nM 7.40
CHEMBL3109987 — IC50 = 40.0 nM 7.40
CHEMBL3110000 — IC50 = 40.0 nM 7.40
CHEMBL3110015 — IC50 = 50.0 nM 7.30
CHEMBL3110020 — IC50 = 50.0 nM 7.30
CHEMBL3110014 — IC50 = 60.0 nM 7.22
CHEMBL3110019 — IC50 = 60.0 nM 7.22
CHEMBL3109986 — IC50 = 60.0 nM 7.22
CHEMBL3110002 — IC50 = 80.0 nM 7.10
CHEMBL3110012 — IC50 = 80.0 nM 7.10
CHEMBL3110018 — IC50 = 100.0 nM 7.00
CHEMBL3110016 — IC50 = 100.0 nM 7.00
CHEMBL3109988 — IC50 = 100.0 nM 7.00
CHEMBL3110013 — IC50 = 100.0 nM 7.00
CHEMBL3110004 — IC50 = 130.0 nM 6.89
CHEMBL3110010 — IC50 = 150.0 nM 6.82
CHEMBL3110011 — IC50 = 150.0 nM 6.82
CHEMBL3109998 — IC50 = 200.0 nM 6.70
CHEMBL3109995 — IC50 = 230.0 nM 6.64
CHEMBL396097 — IC50 = 250.0 nM 6.60
CHEMBL3109992 — IC50 = 280.0 nM 6.55
CHEMBL3110017 — IC50 = 290.0 nM 6.54
CHEMBL3109994 — IC50 = 300.0 nM 6.52
CHEMBL3110003 — IC50 = 310.0 nM 6.51
CHEMBL3110009 — IC50 = 330.0 nM 6.48
CHEMBL3108793 — IC50 = 340.0 nM 6.47
CHEMBL3110005 — IC50 = 340.0 nM 6.47
CHEMBL3109991 — IC50 = 500.0 nM 6.30
CHEMBL3110024 — IC50 = 530.0 nM 6.28
CHEMBL3110023 — IC50 = 540.0 nM 6.27
CHEMBL3109997 — IC50 = 670.0 nM 6.17
CHEMBL3109990 — IC50 = 1100.0 nM 5.96
CHEMBL3109996 — IC50 = 1500.0 nM 5.82
CHEMBL3109989 — IC50 = 1800.0 nM 5.75
CHEMBL3110022 — IC50 = 9000.0 nM 5.05
CHEMBL98 VORINOSTAT IC50 = 41000.0 nM 4.39
CHEMBL3110007 — IC50 = 51000.0 nM 4.29