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Assay Detail

CHEMBL655073

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

Binding
Beta-Trypsin inhibitory activity of compound was determined
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypsin-3 (CHEMBL4551)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.
Costanzo MJ, Yabut SC, Almond HR, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D, Maryanoff BE.
J Med Chem (2003) 46 : 3865 -3876
PubMed 12930148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.50 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124809 1 9.00
CHEMBL340098 1 8.70
CHEMBL127185 1 8.40
CHEMBL339703 1 8.30
CHEMBL341148 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124809 IC50 = 1.0 nM 9.00
CHEMBL340098 IC50 = 2.0 nM 8.70
CHEMBL127185 IC50 = 4.0 nM 8.40
CHEMBL339703 IC50 = 5.0 nM 8.30
CHEMBL341148 IC50 = 8.0 nM 8.10