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Assay Detail

CHEMBL660641

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

Binding
Inhibitory concentration against recombinant human cathepsin L was determined in a fluorescence assay using 5 uM Cbz-Phe-Arg-AMC as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH, Wright LL.
Bioorg Med Chem Lett (2004) 14 : 3425 -3429
PubMed 15177446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.31 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114462 1 7.82
CHEMBL116779 1 6.96
CHEMBL116402 1 6.57
CHEMBL114161 1 6.13
CHEMBL116724 1 5.92
CHEMBL117658 1 5.70
CHEMBL117144 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114462 IC50 = 15.0 nM 7.82
CHEMBL116779 IC50 = 110.0 nM 6.96
CHEMBL116402 IC50 = 270.0 nM 6.57
CHEMBL114161 IC50 = 740.0 nM 6.13
CHEMBL116724 IC50 = 1200.0 nM 5.92
CHEMBL117658 IC50 = 2000.0 nM 5.70
CHEMBL117144 IC50 = 8500.0 nM 5.07