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Assay Detail

CHEMBL2213245

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

Binding
Inhibition of cathepsin L using FR-aminoluciferin as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay
17
Total Activities
17
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 cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Moss N, Xiong Z, Burke M, Cogan D, Gao DA, Haverty K, Heim-Riether A, Hickey ER, Nagaraja R, Netherton M, O'Shea K, Ramsden P, Schwartz R, Shih DT, Ward Y, Young E, Zhang Q.
Bioorg Med Chem Lett (2012) 22 : 7189 -7193
PubMed 23084902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.26 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207571 1 7.30
CHEMBL251327 1 7.21
CHEMBL2207570 1 6.89
CHEMBL2207560 1 6.70
CHEMBL249915 1 6.64
CHEMBL2207564 1 6.40
CHEMBL2207569 1 6.30
CHEMBL2207562 1 6.22
CHEMBL1236882 1 6.00
CHEMBL2207565 1 6.00
CHEMBL2207568 1 5.89
CHEMBL2207567 1 5.05
CHEMBL2207563 1 4.75
CHEMBL387191 1 -
CHEMBL2207561 1 -
CHEMBL2207566 1 -
CHEMBL2207559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207571 IC50 = 50.0 nM 7.30
CHEMBL251327 IC50 = 62.0 nM 7.21
CHEMBL2207570 IC50 = 130.0 nM 6.89
CHEMBL2207560 IC50 = 200.0 nM 6.70
CHEMBL249915 IC50 = 230.0 nM 6.64
CHEMBL2207564 IC50 = 400.0 nM 6.40
CHEMBL2207569 IC50 = 500.0 nM 6.30
CHEMBL2207562 IC50 = 600.0 nM 6.22
CHEMBL1236882 IC50 = 990.0 nM 6.00
CHEMBL2207565 IC50 = 1000.0 nM 6.00
CHEMBL2207568 IC50 = 1300.0 nM 5.89
CHEMBL2207567 IC50 = 9000.0 nM 5.05
CHEMBL2207563 IC50 = 18000.0 nM 4.75
CHEMBL387191 IC50 > 20000.0 nM -
CHEMBL2207561 IC50 > 20000.0 nM -
CHEMBL2207566 IC50 > 20000.0 nM -
CHEMBL2207559 IC50 > 20000.0 nM -