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Assay Detail

CHEMBL920646

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

Binding
Inhibition of Plasmodium falciparum recombinant falcipain-2
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Falcipain 2 (CHEMBL5800)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.
Chipeleme A, Gut J, Rosenthal PJ, Chibale K.
Bioorg Med Chem (2007) 15 : 273 -282
PubMed 17052908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.49 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434743 1 6.20
CHEMBL223654 1 6.14
CHEMBL224312 1 5.65
CHEMBL225449 1 5.58
CHEMBL224025 1 5.50
CHEMBL225646 1 5.42
CHEMBL224893 1 5.23
CHEMBL225323 1 4.96
CHEMBL225184 1 4.74
CHEMBL224258 1 -
CHEMBL387974 1 -
CHEMBL225644 1 -
CHEMBL225592 1 -
CHEMBL388317 1 -
CHEMBL427253 1 -
CHEMBL388101 1 -
CHEMBL224260 1 -
CHEMBL387860 1 -
CHEMBL224891 1 -
CHEMBL389869 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434743 IC50 = 630.0 nM 6.20
CHEMBL223654 IC50 = 720.0 nM 6.14
CHEMBL224312 IC50 = 2250.0 nM 5.65
CHEMBL225449 IC50 = 2600.0 nM 5.58
CHEMBL224025 IC50 = 3160.0 nM 5.50
CHEMBL225646 IC50 = 3800.0 nM 5.42
CHEMBL224893 IC50 = 5850.0 nM 5.23
CHEMBL225323 IC50 = 11070.0 nM 4.96
CHEMBL225184 IC50 = 18220.0 nM 4.74
CHEMBL224258 IC50 > 20000.0 nM -
CHEMBL387974 IC50 > 20000.0 nM -
CHEMBL225644 IC50 > 20000.0 nM -
CHEMBL225592 IC50 > 20000.0 nM -
CHEMBL388317 IC50 > 20000.0 nM -
CHEMBL427253 IC50 > 20000.0 nM -
CHEMBL388101 IC50 > 20000.0 nM -
CHEMBL224260 IC50 > 20000.0 nM -
CHEMBL387860 IC50 > 20000.0 nM -
CHEMBL224891 IC50 > 20000.0 nM -
CHEMBL389869 IC50 > 20000.0 nM -