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Assay Detail

CHEMBL5155335

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

Binding
Inhibition of human recombinant Cathepsin B assessed as Apparent inhibition constant using Z-FR-AMC as substrate inubated 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
Ki 5 6.43 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541700 GALLINAMIDE A 1 6.93
CHEMBL4596647 1 6.62
CHEMBL4598338 1 6.46
CHEMBL4594870 1 6.07
CHEMBL4594757 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541700 GALLINAMIDE A Ki = 117.0 nM 6.93
CHEMBL4596647 Ki = 238.0 nM 6.62
CHEMBL4598338 Ki = 347.0 nM 6.46
CHEMBL4594870 Ki = 861.0 nM 6.07
CHEMBL4594757 Ki = 854.0 nM 6.07