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Assay Detail

CHEMBL921164

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

Binding
Inhibition of HDAC1 in rat liver extract
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL2915)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).
Schäfer S, Saunders L, Eliseeva E, Velena A, Jung M, Schwienhorst A, Strasser A, Dickmanns A, Ficner R, Schlimme S, Sippl W, Verdin E, Jung M.
Bioorg Med Chem (2008) 16 : 2011 -2033
PubMed 18054239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.95 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360194 1 7.68
CHEMBL259517 1 6.89
CHEMBL140000 1 6.62
CHEMBL113003 1 6.36
CHEMBL261492 1 6.24
CHEMBL259708 1 6.23
CHEMBL259434 1 6.20
CHEMBL261272 1 5.78
CHEMBL260080 1 5.68
CHEMBL261587 1 5.61
CHEMBL409860 1 5.59
CHEMBL264411 1 5.52
CHEMBL264926 1 5.52
CHEMBL406734 1 5.50
CHEMBL409526 1 5.50
CHEMBL427776 1 5.12
CHEMBL259826 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360194 IC50 = 21.0 nM 7.68
CHEMBL259517 IC50 = 130.0 nM 6.89
CHEMBL140000 IC50 = 240.0 nM 6.62
CHEMBL113003 IC50 = 440.0 nM 6.36
CHEMBL261492 IC50 = 570.0 nM 6.24
CHEMBL259708 IC50 = 590.0 nM 6.23
CHEMBL259434 IC50 = 630.0 nM 6.20
CHEMBL261272 IC50 = 1680.0 nM 5.78
CHEMBL260080 IC50 = 2110.0 nM 5.68
CHEMBL261587 IC50 = 2440.0 nM 5.61
CHEMBL409860 IC50 = 2550.0 nM 5.59
CHEMBL264411 IC50 = 3030.0 nM 5.52
CHEMBL264926 IC50 = 3010.0 nM 5.52
CHEMBL406734 IC50 = 3190.0 nM 5.50
CHEMBL409526 IC50 = 3180.0 nM 5.50
CHEMBL427776 IC50 = 7530.0 nM 5.12
CHEMBL259826 IC50 = 8760.0 nM 5.06