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Assay Detail

CHEMBL5158467

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

Binding
Inhibition of Cathepsin E (unknown origin) using Mca-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate incubated for 120 mins by fluorescence assay
9
Total Activities
9
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

Cathepsin E (CHEMBL3092)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability.
Li Z, Li H, Jiang F, Wang Z, Zhang W.
Bioorg Med Chem (2022) 57 : 116646 -116646
PubMed 35121401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.58 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296588 PEPSTATIN 2.0 1 9.35
CHEMBL2181022 1 9.14
CHEMBL5184529 1 7.92
CHEMBL2181015 1 7.18
CHEMBL5184180 1 7.00
CHEMBL5184970 1 6.98
CHEMBL5192597 1 6.98
CHEMBL5179569 1 6.92
CHEMBL5188873 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296588 PEPSTATIN IC50 = 0.446 nM 9.35
CHEMBL2181022 IC50 = 0.724 nM 9.14
CHEMBL5184529 IC50 = 12.04 nM 7.92
CHEMBL2181015 IC50 = 66.0 nM 7.18
CHEMBL5184180 IC50 = 100.0 nM 7.00
CHEMBL5184970 IC50 = 105.0 nM 6.98
CHEMBL5192597 IC50 = 104.0 nM 6.98
CHEMBL5179569 IC50 = 120.0 nM 6.92
CHEMBL5188873 IC50 = 187.0 nM 6.73