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Assay Detail

CHEMBL1285768

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Binding
Inhibition of Plasmodium falciparum recombinant falcipain-2
13
Total Activities
13
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

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity.
Gibbons P, Verissimo E, Araujo NC, Barton V, Nixon GL, Amewu RK, Chadwick J, Stocks PA, Biagini GA, Srivastava A, Rosenthal PJ, Gut J, Guedes RC, Moreira R, Sharma R, Berry N, Cristiano ML, Shone AE, Ward SA, O'Neill PM.
J Med Chem (2010) 53 : 8202 -8206
PubMed 20979352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.38 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1277432 1 8.85
CHEMBL1277524 1 7.79
CHEMBL3084785 1 6.37
CHEMBL1277712 1 6.36
CHEMBL3084790 1 6.29
CHEMBL3084787 1 5.92
CHEMBL1277711 1 5.71
CHEMBL1277618 1 5.71
CHEMBL327290 1 5.69
CHEMBL100095 1 5.15
CHEMBL3084786 1 -
CHEMBL3084788 1 -
CHEMBL3084789 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1277432 IC50 = 1.4 nM 8.85
CHEMBL1277524 IC50 = 16.3 nM 7.79
CHEMBL3084785 IC50 = 425.3 nM 6.37
CHEMBL1277712 IC50 = 437.7 nM 6.36
CHEMBL3084790 IC50 = 510.23 nM 6.29
CHEMBL3084787 IC50 = 1200.0 nM 5.92
CHEMBL1277711 IC50 = 1961.0 nM 5.71
CHEMBL1277618 IC50 = 1966.0 nM 5.71
CHEMBL327290 IC50 = 2048.5 nM 5.69
CHEMBL100095 IC50 = 7149.5 nM 5.15
CHEMBL3084786 IC50 < 11500.0 nM -
CHEMBL3084788 IC50 < 8668.0 nM -
CHEMBL3084789 IC50 < 8583.0 nM -