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Assay Detail

CHEMBL4041119

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

Binding
Inhibition of human cathepsin L using Cbz-Phe-Arg-AMC as substrate after 10 mins by fluorescence assay
17
Total Activities
17
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

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).
Previti S, Ettari R, Cosconati S, Amendola G, Chouchene K, Wagner A, Hellmich UA, Ulrich K, Krauth-Siegel RL, Wich PR, Schmid I, Schirmeister T, Gut J, Rosenthal PJ, Grasso S, Zappalà M.
J Med Chem (2017) 60 : 6911 -6923
PubMed 28763614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.58 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078345 1 9.40
CHEMBL4083754 1 9.21
CHEMBL4062015 1 8.66
CHEMBL4096388 1 8.46
CHEMBL4093034 1 7.60
CHEMBL4082758 1 7.57
CHEMBL374508 E-64 1 7.52
CHEMBL4101714 1 7.40
CHEMBL4100751 1 7.39
CHEMBL4081250 1 7.35
CHEMBL4072275 1 6.96
CHEMBL4060936 1 6.62
CHEMBL4070637 1 6.60
CHEMBL2402204 1 6.54
CHEMBL4099269 1 6.48
CHEMBL4090306 1 -
CHEMBL4074432 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078345 Ki = 0.4 nM 9.40
CHEMBL4083754 Ki = 0.61 nM 9.21
CHEMBL4062015 Ki = 2.2 nM 8.66
CHEMBL4096388 Ki = 3.5 nM 8.46
CHEMBL4093034 Ki = 25.0 nM 7.60
CHEMBL4082758 Ki = 27.0 nM 7.57
CHEMBL374508 E-64 Ki = 30.0 nM 7.52
CHEMBL4101714 Ki = 40.0 nM 7.40
CHEMBL4100751 Ki = 41.0 nM 7.39
CHEMBL4081250 Ki = 45.0 nM 7.35
CHEMBL4072275 Ki = 110.0 nM 6.96
CHEMBL4060936 Ki = 240.0 nM 6.62
CHEMBL4070637 Ki = 250.0 nM 6.60
CHEMBL2402204 Ki = 290.0 nM 6.54
CHEMBL4099269 Ki = 330.0 nM 6.48
CHEMBL4090306 Ki - -
CHEMBL4074432 Ki - -