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Assay Detail

CHEMBL3388290

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

Binding
Inhibition of Plasmodium falciparum FP3 using Z-Phe-Arg-AMC as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorescence assay
18
Total Activities
18
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

Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
Conroy T, Guo JT, Elias N, Cergol KM, Gut J, Legac J, Khatoon L, Liu Y, McGowan S, Rosenthal PJ, Hunt NH, Payne RJ.
J Med Chem (2014) 57 : 10557 -10563
PubMed 25412465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.34 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358143 1 7.18
CHEMBL3358142 1 7.09
CHEMBL3358141 1 6.88
CHEMBL3358129 1 6.79
CHEMBL3352874 1 6.74
CHEMBL3358144 1 6.71
CHEMBL3358140 1 6.65
CHEMBL3358128 1 6.54
CHEMBL3358135 1 4.47
CHEMBL3358137 1 4.34
CHEMBL3358133 1 -
CHEMBL3358132 1 -
CHEMBL3358131 1 -
CHEMBL3358130 1 -
CHEMBL3358134 1 -
CHEMBL3358139 1 -
CHEMBL3358136 1 -
CHEMBL3358138 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358143 IC50 = 66.7 nM 7.18
CHEMBL3358142 IC50 = 81.4 nM 7.09
CHEMBL3358141 IC50 = 131.0 nM 6.88
CHEMBL3358129 IC50 = 163.0 nM 6.79
CHEMBL3352874 IC50 = 182.0 nM 6.74
CHEMBL3358144 IC50 = 196.0 nM 6.71
CHEMBL3358140 IC50 = 225.0 nM 6.65
CHEMBL3358128 IC50 = 292.0 nM 6.54
CHEMBL3358135 IC50 = 34000.0 nM 4.47
CHEMBL3358137 IC50 = 46000.0 nM 4.34
CHEMBL3358133 IC50 > 50000.0 nM -
CHEMBL3358132 IC50 > 25000.0 nM -
CHEMBL3358131 IC50 > 50000.0 nM -
CHEMBL3358130 IC50 > 50000.0 nM -
CHEMBL3358134 IC50 > 25000.0 nM -
CHEMBL3358139 IC50 > 50000.0 nM -
CHEMBL3358136 IC50 > 25000.0 nM -
CHEMBL3358138 IC50 > 50000.0 nM -