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Assay Detail

CHEMBL5527359

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

Binding
Inhibition of recombinant Plasmodium falciparum SUB1 using Ac-CKITAQDDEESC-OH as fluorogenic substrate pre-incubated for 5 mins followed by substrate addition and measured every 3 mins for 60 mins by fluorescence based SpectraMax M5e plate reader
21
Total Activities
21
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

Subtilisin-like protease 1 (CHEMBL2052035)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Peptidic Boronic Acid <i>Plasmodium falciparum</i> SUB1 Inhibitors with Improved Selectivity over Human Proteasome.
Withers-Martinez C, Lidumniece E, Hackett F, Collins CR, Taha Z, Blackman MJ, Jirgensons A.
J Med Chem (2024) 67 : 13033 -13055
PubMed 39051854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.10 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5568491 1 8.70
CHEMBL5561987 1 8.68
CHEMBL5532138 1 8.55
CHEMBL5561563 1 8.49
CHEMBL5563634 1 8.47
CHEMBL5560073 1 8.41
CHEMBL5561245 1 8.41
CHEMBL5562881 1 8.27
CHEMBL5564605 1 8.17
CHEMBL5565717 1 8.16
CHEMBL5561949 1 8.16
CHEMBL5563835 1 8.12
CHEMBL5559405 1 8.11
CHEMBL5556185 1 8.03
CHEMBL5567696 1 8.02
CHEMBL5562284 1 7.88
CHEMBL5567647 1 7.82
CHEMBL5561366 1 7.63
CHEMBL5561760 1 7.44
CHEMBL5555306 1 7.36
CHEMBL5565877 1 7.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5568491 IC50 = 2.0 nM 8.70
CHEMBL5561987 IC50 = 2.1 nM 8.68
CHEMBL5532138 IC50 = 2.8 nM 8.55
CHEMBL5561563 IC50 = 3.2 nM 8.49
CHEMBL5563634 IC50 = 3.4 nM 8.47
CHEMBL5560073 IC50 = 3.9 nM 8.41
CHEMBL5561245 IC50 = 3.9 nM 8.41
CHEMBL5562881 IC50 = 5.4 nM 8.27
CHEMBL5564605 IC50 = 6.7 nM 8.17
CHEMBL5565717 IC50 = 6.9 nM 8.16
CHEMBL5561949 IC50 = 6.9 nM 8.16
CHEMBL5563835 IC50 = 7.5 nM 8.12
CHEMBL5559405 IC50 = 7.8 nM 8.11
CHEMBL5556185 IC50 = 9.3 nM 8.03
CHEMBL5567696 IC50 = 9.5 nM 8.02
CHEMBL5562284 IC50 = 13.2 nM 7.88
CHEMBL5567647 IC50 = 15.3 nM 7.82
CHEMBL5561366 IC50 = 23.2 nM 7.63
CHEMBL5561760 IC50 = 36.1 nM 7.44
CHEMBL5555306 IC50 = 43.5 nM 7.36
CHEMBL5565877 IC50 = 71.0 nM 7.15