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Assay Detail

CHEMBL991605

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

Functional
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 in type O+ human erythrocytes after 48 hrs as reduced [3H]hypoxanthine uptake
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.
Hidaka K, Kimura T, Ruben AJ, Uemura T, Kamiya M, Kiso A, Okamoto T, Tsuchiya Y, Hayashi Y, Freire E, Kiso Y.
Bioorg Med Chem (2008) 16 : 10049 -10060
PubMed 18952439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 5.87 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508668 1 6.52
CHEMBL507484 1 6.37
CHEMBL501972 1 6.35
CHEMBL452725 1 6.31
CHEMBL444759 1 6.30
CHEMBL502445 1 6.27
CHEMBL449918 1 6.14
CHEMBL448631 1 5.96
CHEMBL504596 1 5.92
CHEMBL499762 1 5.85
CHEMBL508023 1 5.55
CHEMBL509473 1 5.54
CHEMBL509191 1 5.48
CHEMBL503181 1 5.48
CHEMBL500010 1 5.38
CHEMBL510300 1 5.28
CHEMBL231522 1 5.17
CHEMBL499956 1 -
CHEMBL442632 1 -
CHEMBL448977 1 -
CHEMBL448365 1 -
CHEMBL509323 1 -
CHEMBL452345 1 -
CHEMBL508116 1 -
CHEMBL453415 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508668 EC50 = 300.0 nM 6.52
CHEMBL507484 EC50 = 430.0 nM 6.37
CHEMBL501972 EC50 = 450.0 nM 6.35
CHEMBL452725 EC50 = 490.0 nM 6.31
CHEMBL444759 EC50 = 500.0 nM 6.30
CHEMBL502445 EC50 = 540.0 nM 6.27
CHEMBL449918 EC50 = 720.0 nM 6.14
CHEMBL448631 EC50 = 1100.0 nM 5.96
CHEMBL504596 EC50 = 1200.0 nM 5.92
CHEMBL499762 EC50 = 1400.0 nM 5.85
CHEMBL508023 EC50 = 2800.0 nM 5.55
CHEMBL509473 EC50 = 2900.0 nM 5.54
CHEMBL509191 EC50 = 3300.0 nM 5.48
CHEMBL503181 EC50 = 3300.0 nM 5.48
CHEMBL500010 EC50 = 4200.0 nM 5.38
CHEMBL510300 EC50 = 5200.0 nM 5.28
CHEMBL231522 EC50 = 6800.0 nM 5.17
CHEMBL499956 EC50 > 8000.0 nM -
CHEMBL442632 EC50 > 8000.0 nM -
CHEMBL448977 EC50 > 8000.0 nM -
CHEMBL448365 EC50 > 8000.0 nM -
CHEMBL509323 EC50 > 8000.0 nM -
CHEMBL452345 EC50 > 8000.0 nM -
CHEMBL508116 EC50 > 8000.0 nM -
CHEMBL453415 EC50 > 8000.0 nM -