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Assay Detail

CHEMBL4357657

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Binding
Inhibition of recombinant Plasmodium falciparum Plasmepsin 1
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Plasmepsin I (CHEMBL4687)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).
Cheuka PM, Dziwornu G, Okombo J, Chibale K.
J Med Chem (2020) 63 : 4445 -4467
PubMed 31913032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.55 7.30
Ki 1 9.10 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176888 1 9.10
CHEMBL4225824 1 7.30
CHEMBL4556003 1 7.00
CHEMBL4537622 1 6.98
CHEMBL4530972 1 6.95
CHEMBL4470715 1 6.91
CHEMBL4516552 1 6.55
CHEMBL1233569 1 6.18
CHEMBL1230705 1 5.95
CHEMBL4543535 1 5.93
CHEMBL4435432 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176888 Ki = 0.8 nM 9.10
CHEMBL4225824 IC50 = 50.0 nM 7.30
CHEMBL4556003 IC50 = 100.0 nM 7.00
CHEMBL4537622 IC50 = 104.0 nM 6.98
CHEMBL4530972 IC50 = 113.0 nM 6.95
CHEMBL4470715 IC50 = 123.0 nM 6.91
CHEMBL4516552 IC50 = 280.0 nM 6.55
CHEMBL1233569 IC50 = 655.0 nM 6.18
CHEMBL1230705 IC50 = 1123.0 nM 5.95
CHEMBL4543535 IC50 = 1162.0 nM 5.93
CHEMBL4435432 IC50 = 2000.0 nM 5.70