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Assay Detail

CHEMBL869801

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

Binding
Binding affinity to human tryptase beta2
18
Total Activities
18
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

Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Sperandio D, Tai VW, Lohman J, Hirschbein B, Mendonca R, Lee CS, Spencer JR, Janc J, Nguyen M, Beltman J, Sprengeler P, Scheerens H, Lin T, Liu L, Gadre A, Kellogg A, Green MJ, McGrath ME.
Bioorg Med Chem Lett (2006) 16 : 4085 -4089
PubMed 16725321 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.30 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL211561 1 8.27
CHEMBL212096 1 8.00
CHEMBL426330 1 7.92
CHEMBL208895 1 7.89
CHEMBL215486 1 7.85
CHEMBL212196 1 7.80
CHEMBL212095 1 7.72
CHEMBL210055 1 7.62
CHEMBL209852 1 7.60
CHEMBL380012 1 7.57
CHEMBL265253 1 7.39
CHEMBL211082 1 7.11
CHEMBL377629 1 7.02
CHEMBL214222 1 6.92
CHEMBL210054 1 6.75
CHEMBL383868 1 6.44
CHEMBL210058 1 5.96
CHEMBL214315 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL211561 Ki = 5.4 nM 8.27
CHEMBL212096 Ki = 10.0 nM 8.00
CHEMBL426330 Ki = 12.0 nM 7.92
CHEMBL208895 Ki = 13.0 nM 7.89
CHEMBL215486 Ki = 14.0 nM 7.85
CHEMBL212196 Ki = 16.0 nM 7.80
CHEMBL212095 Ki = 19.0 nM 7.72
CHEMBL210055 Ki = 24.0 nM 7.62
CHEMBL209852 Ki = 25.0 nM 7.60
CHEMBL380012 Ki = 27.0 nM 7.57
CHEMBL265253 Ki = 41.0 nM 7.39
CHEMBL211082 Ki = 78.0 nM 7.11
CHEMBL377629 Ki = 96.0 nM 7.02
CHEMBL214222 Ki = 120.0 nM 6.92
CHEMBL210054 Ki = 180.0 nM 6.75
CHEMBL383868 Ki = 360.0 nM 6.44
CHEMBL210058 Ki = 1100.0 nM 5.96
CHEMBL214315 Ki = 2700.0 nM 5.57