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Assay Detail

CHEMBL4041125

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

Functional
Antiparasitic activity against Plasmodium falciparum W2 after 48 hrs by YOYO-1 probe-based flow cytometry
18
Total Activities
18
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

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).
Previti S, Ettari R, Cosconati S, Amendola G, Chouchene K, Wagner A, Hellmich UA, Ulrich K, Krauth-Siegel RL, Wich PR, Schmid I, Schirmeister T, Gut J, Rosenthal PJ, Grasso S, Zappalà M.
J Med Chem (2017) 60 : 6911 -6923
PubMed 28763614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.85 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 7.64
CHEMBL76 CHLOROQUINE 4.0 1 7.24
CHEMBL4083754 1 5.82
CHEMBL4070637 1 5.64
CHEMBL4096388 1 5.56
CHEMBL4072275 1 5.50
CHEMBL4100751 1 5.40
CHEMBL4101714 1 5.36
CHEMBL4078345 1 5.15
CHEMBL4062015 1 5.14
CHEMBL4093034 1 -
CHEMBL2402204 1 -
CHEMBL4081250 1 -
CHEMBL4099269 1 -
CHEMBL4090306 1 -
CHEMBL4060936 1 -
CHEMBL4074432 1 -
CHEMBL4082758 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ EC50 = 23.0 nM 7.64
CHEMBL76 CHLOROQUINE EC50 = 57.0 nM 7.24
CHEMBL4083754 EC50 = 1530.0 nM 5.82
CHEMBL4070637 EC50 = 2310.0 nM 5.64
CHEMBL4096388 EC50 = 2740.0 nM 5.56
CHEMBL4072275 EC50 = 3160.0 nM 5.50
CHEMBL4100751 EC50 = 3970.0 nM 5.40
CHEMBL4101714 EC50 = 4400.0 nM 5.36
CHEMBL4078345 EC50 = 7030.0 nM 5.15
CHEMBL4062015 EC50 = 7180.0 nM 5.14
CHEMBL4093034 EC50 > 10000.0 nM -
CHEMBL2402204 EC50 > 10000.0 nM -
CHEMBL4081250 EC50 > 10000.0 nM -
CHEMBL4099269 EC50 > 10000.0 nM -
CHEMBL4090306 EC50 > 10000.0 nM -
CHEMBL4060936 EC50 > 10000.0 nM -
CHEMBL4074432 EC50 > 10000.0 nM -
CHEMBL4082758 EC50 > 10000.0 nM -