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Assay Detail

CHEMBL3241235

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Binding
Inhibition of Plasmodium falciparum HSP90 K313Q mutant expressed in yeast assessed as growth inhibition of host after 72 hrs
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Heat-shock protein (CHEMBL4296306)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors.
Wang T, Bisson WH, Mäser P, Scapozza L, Picard D.
J Med Chem (2014) 57 : 2524 -2535
PubMed 24580531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.61 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109480 TANESPIMYCIN 3.0 1 4.70
CHEMBL3234416 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109480 TANESPIMYCIN IC50 = 20100.0 nM 4.70
CHEMBL3234416 IC50 = 31100.0 nM 4.51