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Assay Detail

CHEMBL5320640

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

Binding
Inhibition of human cathepsin K using Z-LR-AMC as substrate preincubated for 20 mins followed by pre-activated enzyme addition and measured after 15 mins by fluorescence based microplate reader analysis
8
Total Activities
8
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 K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
Behring L, Ruiz-Gómez G, Trapp C, Morales M, Wodtke R, Köckerling M, Kopka K, Pisabarro MT, Pietzsch J, Löser R.
J Med Chem (2023) 66 : 3818 -3851
PubMed 36867428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.89 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5405909 1 5.68
CHEMBL5395533 1 5.40
CHEMBL5411088 1 5.05
CHEMBL5401219 1 4.72
CHEMBL5413230 1 4.60
CHEMBL134083 1 4.59
CHEMBL5409217 1 4.58
CHEMBL5432531 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5405909 Ki = 2100.0 nM 5.68
CHEMBL5395533 Ki = 4000.0 nM 5.40
CHEMBL5411088 Ki = 8810.0 nM 5.05
CHEMBL5401219 Ki = 19100.0 nM 4.72
CHEMBL5413230 Ki = 25000.0 nM 4.60
CHEMBL134083 Ki = 25940.0 nM 4.59
CHEMBL5409217 Ki = 26000.0 nM 4.58
CHEMBL5432531 Ki = 30000.0 nM 4.52