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Assay Detail

CHEMBL839534

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

Binding
Inhibitory activity against human mast cell tryptase beta
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 Expert

Target

Tryptase beta-1 (CHEMBL2617)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.
Vaz RJ, Gao Z, Pribish J, Chen X, Levell J, Davis L, Albert E, Brollo M, Ugolini A, Cramer DM, Cairns J, Sides K, Liu F, Kwong J, Kang J, Rebello S, Elliot M, Lim H, Chellaraj V, Singleton RW, Li Y.
Bioorg Med Chem Lett (2004) 14 : 6053 -6056
PubMed 15546728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.07 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365062 1 8.89
CHEMBL362874 1 8.82
CHEMBL186730 1 8.37
CHEMBL185752 1 7.23
CHEMBL188068 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365062 Ki = 1.3 nM 8.89
CHEMBL362874 Ki = 1.5 nM 8.82
CHEMBL186730 Ki = 4.3 nM 8.37
CHEMBL185752 Ki = 59.0 nM 7.23
CHEMBL188068 Ki = 88.0 nM 7.06