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Assay Detail

CHEMBL4121605

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

Binding
Inhibition of human cathepsin L using Z-L-R-AMC as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by spectrophotometric method
27
Total Activities
27
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

Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.
Zwicker JD, Diaz NA, Guerra AJ, Kirchhoff PD, Wen B, Sun D, Carruthers VB, Larsen SD.
Bioorg Med Chem Lett (2018) 28 : 1972 -1980
PubMed 29650289 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.76 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222649 1 8.52
CHEMBL4129611 1 7.82
CHEMBL4126611 1 7.38
CHEMBL565079 1 7.36
CHEMBL4128244 1 7.32
CHEMBL4125776 1 7.11
CHEMBL4128887 1 7.08
CHEMBL4127007 1 7.07
CHEMBL4126455 1 7.04
CHEMBL4126546 1 7.03
CHEMBL4130028 1 6.96
CHEMBL4129470 1 6.96
CHEMBL4129884 1 6.89
CHEMBL4126741 1 6.85
CHEMBL4130249 1 6.85
CHEMBL4126824 1 6.72
CHEMBL4127142 1 6.62
CHEMBL4128116 1 6.55
CHEMBL4130087 1 6.55
CHEMBL4126172 1 6.50
CHEMBL4129822 1 6.23
CHEMBL4126675 1 5.92
CHEMBL4129022 1 5.92
CHEMBL4127618 1 5.60
CHEMBL4128869 1 5.46
CHEMBL4130234 1 5.39
CHEMBL4128058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222649 IC50 = 3.0 nM 8.52
CHEMBL4129611 IC50 = 15.0 nM 7.82
CHEMBL4126611 IC50 = 42.0 nM 7.38
CHEMBL565079 IC50 = 44.0 nM 7.36
CHEMBL4128244 IC50 = 48.0 nM 7.32
CHEMBL4125776 IC50 = 77.0 nM 7.11
CHEMBL4128887 IC50 = 84.0 nM 7.08
CHEMBL4127007 IC50 = 86.0 nM 7.07
CHEMBL4126455 IC50 = 92.0 nM 7.04
CHEMBL4126546 IC50 = 93.0 nM 7.03
CHEMBL4130028 IC50 = 110.0 nM 6.96
CHEMBL4129470 IC50 = 110.0 nM 6.96
CHEMBL4129884 IC50 = 130.0 nM 6.89
CHEMBL4126741 IC50 = 140.0 nM 6.85
CHEMBL4130249 IC50 = 140.0 nM 6.85
CHEMBL4126824 IC50 = 190.0 nM 6.72
CHEMBL4127142 IC50 = 240.0 nM 6.62
CHEMBL4128116 IC50 = 280.0 nM 6.55
CHEMBL4130087 IC50 = 280.0 nM 6.55
CHEMBL4126172 IC50 = 320.0 nM 6.50
CHEMBL4129822 IC50 = 590.0 nM 6.23
CHEMBL4126675 IC50 = 1200.0 nM 5.92
CHEMBL4129022 IC50 = 1200.0 nM 5.92
CHEMBL4127618 IC50 = 2500.0 nM 5.60
CHEMBL4128869 IC50 = 3500.0 nM 5.46
CHEMBL4130234 IC50 = 4100.0 nM 5.39
CHEMBL4128058 IC50 = 816000.0 nM -