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Assay Detail

CHEMBL1959442

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

Binding
Inhibition of HDAC1
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
Hirata Y, Hirata M, Kawaratani Y, Shibano M, Taniguchi M, Yasuda M, Ohmomo Y, Nagaoka Y, Baba K, Uesato S.
Bioorg Med Chem Lett (2012) 22 : 1926 -1930
PubMed 22321215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.06 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.22
CHEMBL251819 1 7.40
CHEMBL1957458 1 7.30
CHEMBL1957463 1 7.22
CHEMBL1957459 1 7.10
CHEMBL1957464 1 7.00
CHEMBL27759 ENTINOSTAT 3.0 1 6.32
CHEMBL407420 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 6.0 nM 8.22
CHEMBL251819 IC50 = 40.0 nM 7.40
CHEMBL1957458 IC50 = 50.0 nM 7.30
CHEMBL1957463 IC50 = 60.0 nM 7.22
CHEMBL1957459 IC50 = 80.0 nM 7.10
CHEMBL1957464 IC50 = 100.0 nM 7.00
CHEMBL27759 ENTINOSTAT IC50 = 480.0 nM 6.32
CHEMBL407420 IC50 = 1170.0 nM 5.93