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Assay Detail

CHEMBL817294

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Binding
Inhibition of Tryptase in human mast cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Tryptase (CHEMBL2095193)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
Dener JM, Rice KD, Newcomb WS, Wang VR, Young WB, Gangloff AR, Kuo EY, Cregar L, Putnam D, Wong M.
Bioorg Med Chem Lett (2001) 11 : 1629 -1633
PubMed 11425524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.18 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46809 1 10.15
CHEMBL297220 1 9.40
CHEMBL42900 1 9.30
CHEMBL43938 1 9.07
CHEMBL40491 1 9.04
CHEMBL42898 1 8.95
CHEMBL38054 1 8.17
CHEMBL298256 1 8.06
CHEMBL295007 1 8.05
CHEMBL42899 1 7.80
CHEMBL295450 1 7.79
CHEMBL296733 1 7.62
CHEMBL42037 1 7.55
CHEMBL42364 1 7.39
CHEMBL406192 1 6.96
CHEMBL289918 1 6.95
CHEMBL297408 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46809 Ki = 0.07 nM 10.15
CHEMBL297220 Ki = 0.4 nM 9.40
CHEMBL42900 Ki = 0.5 nM 9.30
CHEMBL43938 Ki = 0.85 nM 9.07
CHEMBL40491 Ki = 0.91 nM 9.04
CHEMBL42898 Ki = 1.12 nM 8.95
CHEMBL38054 Ki = 6.7 nM 8.17
CHEMBL298256 Ki = 8.7 nM 8.06
CHEMBL295007 Ki = 8.9 nM 8.05
CHEMBL42899 Ki = 16.0 nM 7.80
CHEMBL295450 Ki = 16.4 nM 7.79
CHEMBL296733 Ki = 24.0 nM 7.62
CHEMBL42037 Ki = 28.0 nM 7.55
CHEMBL42364 Ki = 40.6 nM 7.39
CHEMBL406192 Ki = 110.0 nM 6.96
CHEMBL289918 Ki = 112.0 nM 6.95
CHEMBL297408 Ki = 155.0 nM 6.81