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Assay Detail

CHEMBL4020982

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

Binding
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
Mehndiratta S, Wang RS, Huang HL, Su CJ, Hsu CM, Wu YW, Pan SL, Liou JP.
Eur J Med Chem (2017) 134 : 13 -23
PubMed 28395150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.55 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080164 1 8.31
CHEMBL4090847 1 8.14
CHEMBL4069853 1 8.07
CHEMBL4065026 1 7.84
CHEMBL4083054 1 7.52
CHEMBL4086475 1 7.28
CHEMBL4066741 1 7.22
CHEMBL4061184 1 7.12
CHEMBL408513 BELINOSTAT 4.0 1 7.09
CHEMBL98 VORINOSTAT 4.0 1 6.88
CHEMBL27759 ENTINOSTAT 3.0 1 -
CHEMBL4091752 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080164 IC50 = 4.9 nM 8.31
CHEMBL4090847 IC50 = 7.17 nM 8.14
CHEMBL4069853 IC50 = 8.56 nM 8.07
CHEMBL4065026 IC50 = 14.3 nM 7.84
CHEMBL4083054 IC50 = 30.45 nM 7.52
CHEMBL4086475 IC50 = 52.17 nM 7.28
CHEMBL4066741 IC50 = 60.0 nM 7.22
CHEMBL4061184 IC50 = 76.13 nM 7.12
CHEMBL408513 BELINOSTAT IC50 = 81.0 nM 7.09
CHEMBL98 VORINOSTAT IC50 = 131.26 nM 6.88
CHEMBL27759 ENTINOSTAT IC50 > 1000.0 nM -
CHEMBL4091752 IC50 > 1000.0 nM -