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Assay Detail

CHEMBL4330016

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

Binding
Inhibition of KLK4 (unknown origin) expressed in sf9 cells using Ac-FVQR-pNA as substrate preincubated for 30 mins followed by substrate addition and measured for 7 mins by spectrophotometric method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kallikrein-4 (CHEMBL4446)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.
Swedberg JE, Ghani HA, Harris JM, de Veer SJ, Craik DJ.
ACS Med Chem Lett (2018) 9 : 1258 -1262
PubMed 30613336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.31 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564063 1 10.00
CHEMBL4543437 1 9.89
CHEMBL4566258 1 9.52
CHEMBL4531700 1 9.36
CHEMBL4452574 1 8.89
CHEMBL4530379 1 8.80
CHEMBL4443340 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564063 Ki = 0.1 nM 10.00
CHEMBL4543437 Ki = 0.13 nM 9.89
CHEMBL4566258 Ki = 0.3 nM 9.52
CHEMBL4531700 Ki = 0.44 nM 9.36
CHEMBL4452574 Ki = 1.3 nM 8.89
CHEMBL4530379 Ki = 1.6 nM 8.80
CHEMBL4443340 Ki = 1.8 nM 8.74