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Assay Detail

CHEMBL5155326

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Binding
Inhibition of human recombinant Cathepsin B assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
Ashhurst AS, Tang AH, Fajtová P, Yoon MC, Aggarwal A, Bedding MJ, Stoye A, Beretta L, Pwee D, Drelich A, Skinner D, Li L, Meek TD, McKerrow JH, Hook V, Tseng CT, Larance M, Turville S, Gerwick WH, O'Donoghue AJ, Payne RJ.
J Med Chem (2022) 65 : 2956 -2970
PubMed 34730959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.13 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541700 GALLINAMIDE A 1 8.13
CHEMBL4594870 1 -
CHEMBL4598338 1 -
CHEMBL4594757 1 -
CHEMBL4596647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541700 GALLINAMIDE A IC50 = 7.34 nM 8.13
CHEMBL4594870 IC50 = 2.78 10^-4microM -
CHEMBL4598338 IC50 = 4.76 10^-2microM -
CHEMBL4594757 IC50 = 4.16 10^-4microM -
CHEMBL4596647 IC50 = 1.49 10^-4microM -