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Assay Detail

CHEMBL3815698

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

Binding
Reversible inhibition of recombinant Plasmodium falciparum falcipain 2 assessed as hydrolysis of Cbz-Phe-Arg-AMC measured after 10 mins by spectrofluorometric method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Bistacrine derivatives as new potent antimalarials.
Schmidt I, Pradel G, Sologub L, Golzmann A, Ngwa CJ, Kucharski A, Schirmeister T, Holzgrabe U.
Bioorg Med Chem (2016) 24 : 3636 -3642
PubMed 27316542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.92 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814557 1 5.28
CHEMBL424707 1 4.94
CHEMBL3815015 1 4.83
CHEMBL75274 1 4.77
CHEMBL73160 1 4.76
CHEMBL3814548 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814557 IC50 = 5200.0 nM 5.28
CHEMBL424707 IC50 = 11500.0 nM 4.94
CHEMBL3815015 IC50 = 14900.0 nM 4.83
CHEMBL75274 IC50 = 17100.0 nM 4.77
CHEMBL73160 IC50 = 17300.0 nM 4.76
CHEMBL3814548 IC50 - -