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Assay Detail

CHEMBL948933

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Binding
Inhibition of kallikrein
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Plasma kallikrein (CHEMBL2000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Maryanoff BE, Costanzo MJ.
Bioorg Med Chem (2008) 16 : 1562 -1595
PubMed 18053726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.64 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413155 1 8.00
CHEMBL270834 1 7.89
CHEMBL414002 1 7.85
CHEMBL271047 1 7.54
CHEMBL256427 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413155 IC50 = 10.0 nM 8.00
CHEMBL270834 IC50 = 13.0 nM 7.89
CHEMBL414002 IC50 = 14.0 nM 7.85
CHEMBL271047 IC50 = 29.0 nM 7.54
CHEMBL256427 IC50 = 120.0 nM 6.92