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Assay Detail

CHEMBL4185201

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

Functional
Antimalarial activity against Plasmodium falciparum infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
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 5 6.88 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 8.00
CHEMBL408513 BELINOSTAT 4.0 1 7.22
CHEMBL343448 ROMIDEPSIN 4.0 1 7.05
CHEMBL320497 SUBEROHYDROXAMIC ACID 1 6.10
CHEMBL4215938 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 10.0 nM 8.00
CHEMBL408513 BELINOSTAT IC50 = 60.0 nM 7.22
CHEMBL343448 ROMIDEPSIN IC50 = 90.0 nM 7.05
CHEMBL320497 SUBEROHYDROXAMIC ACID IC50 = 800.0 nM 6.10
CHEMBL4215938 IC50 = 900.0 nM 6.05