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Assay Detail

CHEMBL4322964

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Binding
Inhibition of human cathepsin L using fluorogenic substrate cbz-FR-AMC monitored for 90 to 120 mins by spectrophotometry
16
Total Activities
16
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

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and <i>Trypanosoma cruzi</i> Cruzain.
Boudreau PD, Miller BW, McCall LI, Almaliti J, Reher R, Hirata K, Le T, Siqueira-Neto JL, Hook V, Gerwick WH.
J Med Chem (2019) 62 : 9026 -9044
PubMed 31539239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.53 10.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441303 1 10.03
CHEMBL4447348 1 9.20
CHEMBL4527930 1 9.10
CHEMBL4582558 1 9.00
CHEMBL4471760 1 8.88
CHEMBL4445744 1 8.87
CHEMBL4474668 1 8.78
CHEMBL4482954 1 8.76
CHEMBL4527867 1 8.50
CHEMBL4475810 1 8.45
CHEMBL4527329 1 8.45
CHEMBL4564747 1 8.38
CHEMBL541700 GALLINAMIDE A 1 8.33
CHEMBL4457500 1 8.18
CHEMBL4514842 1 7.11
CHEMBL4468530 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441303 IC50 = 0.094 nM 10.03
CHEMBL4447348 IC50 = 0.632 nM 9.20
CHEMBL4527930 IC50 = 0.79 nM 9.10
CHEMBL4582558 IC50 = 1.0 nM 9.00
CHEMBL4471760 IC50 = 1.31 nM 8.88
CHEMBL4445744 IC50 = 1.35 nM 8.87
CHEMBL4474668 IC50 = 1.68 nM 8.78
CHEMBL4482954 IC50 = 1.73 nM 8.76
CHEMBL4527867 IC50 = 3.13 nM 8.50
CHEMBL4475810 IC50 = 3.54 nM 8.45
CHEMBL4527329 IC50 = 3.53 nM 8.45
CHEMBL4564747 IC50 = 4.15 nM 8.38
CHEMBL541700 GALLINAMIDE A IC50 = 4.67 nM 8.33
CHEMBL4457500 IC50 = 6.64 nM 8.18
CHEMBL4514842 IC50 = 77.0 nM 7.11
CHEMBL4468530 IC50 = 376.0 nM 6.42