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Assay Detail

CHEMBL4355183

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

Binding
Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay
5
Total Activities
5
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

Kallikrein-5 (CHEMBL4447)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Amino Acid Scanning at P5' within the Bowman-Birk Inhibitory Loop Reveals Specificity Trends for Diverse Serine Proteases.
Li CY, de Veer SJ, White AM, Chen X, Harris JM, Swedberg JE, Craik DJ.
J Med Chem (2019) 62 : 3696 -3706
PubMed 30888159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.74 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4466351 1 9.47
CHEMBL4550494 1 9.14
CHEMBL4575658 1 8.62
CHEMBL4456620 1 8.43
CHEMBL4513520 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4466351 Ki = 0.34 nM 9.47
CHEMBL4550494 Ki = 0.73 nM 9.14
CHEMBL4575658 Ki = 2.4 nM 8.62
CHEMBL4456620 Ki = 3.7 nM 8.43
CHEMBL4513520 Ki = 8.9 nM 8.05