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Assay Detail

CHEMBL4181679

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

Binding
Inhibition of Plasmodium falciparum FP2 using Z-Leu-Arg-AMC as substrate preincubated for 30 min followed by substrate addition measured after 30 mins by spectrofluorimetric method
24
Total Activities
24
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

Cysteine protease falcipain-2 (CHEMBL5801)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
Chen W, Huang Z, Wang W, Mao F, Guan L, Tang Y, Jiang H, Li J, Huang J, Jiang L, Zhu J.
Bioorg Med Chem (2017) 25 : 6467 -6478
PubMed 29111368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.07 5.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211317 1 5.31
CHEMBL4207961 1 5.29
CHEMBL4218177 1 5.21
CHEMBL4218788 1 5.17
CHEMBL1939368 1 5.16
CHEMBL4211543 1 5.13
CHEMBL4203015 1 5.12
CHEMBL4212687 1 5.11
CHEMBL4209200 1 5.04
CHEMBL4209486 1 5.00
CHEMBL4213904 1 5.00
CHEMBL1458713 1 4.24
CHEMBL4210479 1 -
CHEMBL4214368 1 -
CHEMBL4202708 1 -
CHEMBL4210735 1 -
CHEMBL4207059 1 -
CHEMBL4206536 1 -
CHEMBL4213489 1 -
CHEMBL4203128 1 -
CHEMBL4216274 1 -
CHEMBL4213293 1 -
CHEMBL4209975 1 -
CHEMBL36 PYRIMETHAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211317 IC50 = 4900.0 nM 5.31
CHEMBL4207961 IC50 = 5100.0 nM 5.29
CHEMBL4218177 IC50 = 6200.0 nM 5.21
CHEMBL4218788 IC50 = 6700.0 nM 5.17
CHEMBL1939368 IC50 = 7000.0 nM 5.16
CHEMBL4211543 IC50 = 7400.0 nM 5.13
CHEMBL4203015 IC50 = 7600.0 nM 5.12
CHEMBL4212687 IC50 = 7700.0 nM 5.11
CHEMBL4209200 IC50 = 9100.0 nM 5.04
CHEMBL4209486 IC50 = 10000.0 nM 5.00
CHEMBL4213904 IC50 = 10000.0 nM 5.00
CHEMBL1458713 IC50 = 57200.0 nM 4.24
CHEMBL4210479 IC50 - -
CHEMBL4214368 IC50 - -
CHEMBL4202708 IC50 - -
CHEMBL4210735 IC50 - -
CHEMBL4207059 IC50 - -
CHEMBL4206536 IC50 - -
CHEMBL4213489 IC50 - -
CHEMBL4203128 IC50 - -
CHEMBL4216274 IC50 - -
CHEMBL4213293 IC50 - -
CHEMBL4209975 IC50 - -
CHEMBL36 PYRIMETHAMINE IC50 - -