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Assay Detail

CHEMBL839921

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

Binding
In vitro inhibitory activity against tryptase
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
Hopkins CR, Czekaj M, Kaye SS, Gao Z, Pribish J, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Luo Y, Lim HK, Vaz R, Rebello S, Maignan S, Dupuy A, Mathieu M, Levell J.
Bioorg Med Chem Lett (2005) 15 : 2734 -2737
PubMed 15911249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.88 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191546 1 7.50
CHEMBL365527 1 7.39
CHEMBL370284 1 7.39
CHEMBL192963 1 7.31
CHEMBL193514 1 7.24
CHEMBL189101 1 7.21
CHEMBL370463 1 7.17
CHEMBL365148 1 7.00
CHEMBL365189 1 6.94
CHEMBL372028 1 6.91
CHEMBL364661 1 6.90
CHEMBL189531 1 6.89
CHEMBL99951 1 6.85
CHEMBL190103 1 6.85
CHEMBL191007 1 6.81
CHEMBL435694 1 6.79
CHEMBL361040 1 6.73
CHEMBL372912 1 6.71
CHEMBL190000 1 6.62
CHEMBL192214 1 6.61
CHEMBL436537 1 6.54
CHEMBL190135 1 6.51
CHEMBL189983 1 6.43
CHEMBL189372 1 6.43
CHEMBL191731 1 6.30
CHEMBL188104 1 -
CHEMBL191072 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191546 Ki = 32.0 nM 7.50
CHEMBL365527 Ki = 41.0 nM 7.39
CHEMBL370284 Ki = 41.0 nM 7.39
CHEMBL192963 Ki = 49.0 nM 7.31
CHEMBL193514 Ki = 57.0 nM 7.24
CHEMBL189101 Ki = 61.0 nM 7.21
CHEMBL370463 Ki = 68.0 nM 7.17
CHEMBL365148 Ki = 101.0 nM 7.00
CHEMBL365189 Ki = 116.0 nM 6.94
CHEMBL372028 Ki = 124.0 nM 6.91
CHEMBL364661 Ki = 125.0 nM 6.90
CHEMBL189531 Ki = 128.0 nM 6.89
CHEMBL99951 Ki = 140.0 nM 6.85
CHEMBL190103 Ki = 141.0 nM 6.85
CHEMBL191007 Ki = 155.0 nM 6.81
CHEMBL435694 Ki = 162.0 nM 6.79
CHEMBL361040 Ki = 185.0 nM 6.73
CHEMBL372912 Ki = 197.0 nM 6.71
CHEMBL190000 Ki = 240.0 nM 6.62
CHEMBL192214 Ki = 246.0 nM 6.61
CHEMBL436537 Ki = 290.0 nM 6.54
CHEMBL190135 Ki = 310.0 nM 6.51
CHEMBL189983 Ki = 368.0 nM 6.43
CHEMBL189372 Ki = 373.0 nM 6.43
CHEMBL191731 Ki = 497.0 nM 6.30
CHEMBL188104 Ki > 20000.0 nM -
CHEMBL191072 Ki > 20000.0 nM -