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Assay Detail

CHEMBL817299

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

Binding
Inhibitory activity against human tryptase enzyme
30
Total Activities
30
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

Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors.
Dener JM, Wang VR, Rice KD, Gangloff AR, Kuo EY, Newcomb WS, Putnam D, Wong M.
Bioorg Med Chem Lett (2001) 11 : 2325 -2330
PubMed 11527724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 5.70 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46809 1 10.15
CHEMBL297220 1 9.40
CHEMBL75205 1 7.08
CHEMBL306372 1 6.80
CHEMBL74087 1 6.68
CHEMBL72985 1 6.52
CHEMBL309262 1 6.47
CHEMBL309580 1 6.40
CHEMBL74695 1 6.06
CHEMBL76769 1 6.05
CHEMBL305614 1 5.89
CHEMBL310399 1 5.58
CHEMBL310411 1 5.16
CHEMBL311936 1 5.16
CHEMBL73907 1 5.16
CHEMBL77525 1 5.14
CHEMBL305677 1 5.13
CHEMBL311844 1 5.01
CHEMBL74494 1 5.01
CHEMBL75531 1 4.96
CHEMBL74360 1 4.96
CHEMBL74428 1 4.92
CHEMBL76579 1 4.89
CHEMBL74905 1 4.80
CHEMBL308808 1 4.62
CHEMBL74482 1 4.54
CHEMBL76819 1 4.38
CHEMBL308376 1 4.30
CHEMBL305643 1 4.10
CHEMBL77104 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46809 Ki = 0.07 nM 10.15
CHEMBL297220 Ki = 0.4 nM 9.40
CHEMBL75205 Ki = 84.0 nM 7.08
CHEMBL306372 Ki = 160.0 nM 6.80
CHEMBL74087 Ki = 210.0 nM 6.68
CHEMBL72985 Ki = 300.0 nM 6.52
CHEMBL309262 Ki = 340.0 nM 6.47
CHEMBL309580 Ki = 400.0 nM 6.40
CHEMBL74695 Ki = 870.0 nM 6.06
CHEMBL76769 Ki = 890.0 nM 6.05
CHEMBL305614 Ki = 1300.0 nM 5.89
CHEMBL310399 Ki = 2600.0 nM 5.58
CHEMBL310411 Ki = 7000.0 nM 5.16
CHEMBL311936 Ki = 6900.0 nM 5.16
CHEMBL73907 Ki = 6900.0 nM 5.16
CHEMBL77525 Ki = 7300.0 nM 5.14
CHEMBL305677 Ki = 7400.0 nM 5.13
CHEMBL311844 Ki = 9700.0 nM 5.01
CHEMBL74494 Ki = 9800.0 nM 5.01
CHEMBL75531 Ki = 11000.0 nM 4.96
CHEMBL74360 Ki = 11000.0 nM 4.96
CHEMBL74428 Ki = 12000.0 nM 4.92
CHEMBL76579 Ki = 13000.0 nM 4.89
CHEMBL74905 Ki = 16000.0 nM 4.80
CHEMBL308808 Ki = 24000.0 nM 4.62
CHEMBL74482 Ki = 29000.0 nM 4.54
CHEMBL76819 Ki = 42000.0 nM 4.38
CHEMBL308376 Ki = 50000.0 nM 4.30
CHEMBL305643 Ki = 80000.0 nM 4.10
CHEMBL77104 Ki = 370000.0 nM -