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Assay Detail

CHEMBL1219552

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

Binding
Inhibition of Plasmodium falciparum HDAC1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase (CHEMBL5541)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
Mwakwari SC, Guerrant W, Patil V, Khan SI, Tekwani BL, Gurard-Levin ZA, Mrksich M, Oyelere AK.
J Med Chem (2010) 53 : 6100 -6111
PubMed 20669972 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.13 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1214760 1 8.00
CHEMBL1214759 1 7.44
CHEMBL1214761 1 7.40
CHEMBL98 VORINOSTAT 4.0 1 6.89
CHEMBL1214762 1 6.54
CHEMBL1214763 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1214760 IC50 = 10.0 nM 8.00
CHEMBL1214759 IC50 = 36.0 nM 7.44
CHEMBL1214761 IC50 = 40.0 nM 7.40
CHEMBL98 VORINOSTAT IC50 = 130.0 nM 6.89
CHEMBL1214762 IC50 = 290.0 nM 6.54
CHEMBL1214763 IC50 = 304.0 nM 6.52