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Assay Detail

CHEMBL2051700

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

Binding
Inhibition of human recombinant HDAC2 after 30 mins by fluorometric assay
7
Total Activities
7
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
Lai MJ, Huang HL, Pan SL, Liu YM, Peng CY, Lee HY, Yeh TK, Huang PH, Teng CM, Chen CS, Chuang HY, Liou JP.
J Med Chem (2012) 55 : 3777 -3791
PubMed 22439863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.44 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 8.77
CHEMBL2048750 1 8.64
CHEMBL2048746 1 8.40
CHEMBL2048752 1 6.72
CHEMBL2048751 1 6.70
CHEMBL2048749 1 6.44
CHEMBL2048755 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 1.7 nM 8.77
CHEMBL2048750 IC50 = 2.3 nM 8.64
CHEMBL2048746 IC50 = 4.0 nM 8.40
CHEMBL2048752 IC50 = 189.3 nM 6.72
CHEMBL2048751 IC50 = 199.4 nM 6.70
CHEMBL2048749 IC50 = 361.8 nM 6.44
CHEMBL2048755 IC50 = 381.1 nM 6.42