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Assay Detail

CHEMBL4185199

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

Binding
Inhibition of HDAC1 in Plasmodium falciparum 3D7 nuclear extract using Ac-RGK(Ac)-AMC fluorogenic peptide as substrate preincubated for 1 hr followed by substrate addition measured after 10 min by fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum 3D7
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histone deacetylase (CHEMBL5541)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
Hailu GS, Robaa D, Forgione M, Sippl W, Rotili D, Mai A.
J Med Chem (2017) 60 : 4780 -4804
PubMed 28241112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.07 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343448 ROMIDEPSIN 4.0 1 9.05
CHEMBL483254 PANOBINOSTAT 4.0 1 8.48
CHEMBL408513 BELINOSTAT 4.0 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343448 ROMIDEPSIN IC50 = 0.9 nM 9.05
CHEMBL483254 PANOBINOSTAT IC50 = 3.3 nM 8.48
CHEMBL408513 BELINOSTAT IC50 = 214.7 nM 6.67