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Assay Detail

CHEMBL4234763

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
17
Total Activities
16
Compounds Tested
2
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

Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.
Royo S, Schirmeister T, Kaiser M, Jung S, Rodríguez S, Bautista JM, González FV.
Bioorg Med Chem (2018) 26 : 4624 -4634
PubMed 30037754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.26 8.00
Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4238441 1 8.00
CHEMBL4244656 1 8.00
CHEMBL4251480 1 7.30
CHEMBL4240920 1 7.10
CHEMBL4237990 1 7.05
CHEMBL4242138 1 6.75
CHEMBL4249696 1 6.68
CHEMBL4245127 1 6.58
CHEMBL4248915 1 6.30
CHEMBL4244085 2 5.83
CHEMBL4250264 1 5.61
CHEMBL4242650 1 4.88
CHEMBL4246909 1 4.84
CHEMBL4238922 1 4.70
CHEMBL4247075 1 4.33
CHEMBL4247707 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4244656 IC50 = 10.0 nM 8.00
CHEMBL4238441 IC50 = 10.0 nM 8.00
CHEMBL4251480 IC50 = 50.0 nM 7.30
CHEMBL4240920 IC50 = 80.0 nM 7.10
CHEMBL4237990 IC50 = 90.0 nM 7.05
CHEMBL4242138 IC50 = 180.0 nM 6.75
CHEMBL4249696 IC50 = 210.0 nM 6.68
CHEMBL4245127 IC50 = 260.0 nM 6.58
CHEMBL4248915 IC50 = 500.0 nM 6.30
CHEMBL4244085 IC50 = 1490.0 nM 5.83
CHEMBL4250264 IC50 = 2450.0 nM 5.61
CHEMBL4242650 IC50 = 13100.0 nM 4.88
CHEMBL4246909 IC50 = 14300.0 nM 4.84
CHEMBL4238922 IC50 = 20000.0 nM 4.70
CHEMBL4247075 IC50 = 47000.0 nM 4.33
CHEMBL4247707 IC50 > 2000.0 nM -
CHEMBL4244085 Ki = 780000.0 nM -