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Assay Detail

CHEMBL5131159

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

Binding
Inhibition of Plasmodium falciparum 3D7 HA-glms-tagged PMX using DABCYL-HSFIQEGKEE-EDANS as substrate measured after 2 hrs by FRET assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Plasmepsin X (CHEMBL4523390)
Type SINGLE PROTEIN
Organism Plasmodium falciparum (isolate 3D7)

Publication

The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.
de Lera Ruiz M, Favuzza P, Guo Z, Zhao L, Hu B, Lei Z, Zhan D, Murgolo N, Boyce CW, Vavrek M, Thompson J, Ngo A, Jarman KE, Robbins J, Boddey J, Sleebs BE, Lowes KN, Cowman AF, Olsen DB, McCauley JA.
ACS Med Chem Lett (2022) 13 : 1745 -1754
PubMed 36385924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 9.50 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5171401 1 10.52
CHEMBL5182418 1 10.22
CHEMBL5187792 1 10.15
CHEMBL5193119 1 9.52
CHEMBL5199100 1 9.40
CHEMBL5207556 1 9.22
CHEMBL5197877 1 8.72
CHEMBL5178733 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5171401 IC50 = 0.03 nM 10.52
CHEMBL5182418 IC50 = 0.06 nM 10.22
CHEMBL5187792 IC50 = 0.07 nM 10.15
CHEMBL5193119 IC50 = 0.3 nM 9.52
CHEMBL5199100 IC50 = 0.4 nM 9.40
CHEMBL5207556 IC50 = 0.6 nM 9.22
CHEMBL5197877 IC50 = 1.9 nM 8.72
CHEMBL5178733 IC50 = 5.7 nM 8.24