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Assay Detail

CHEMBL824722

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

Binding
Inhibitory potency against trypsin
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine protease 1 (CHEMBL209)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.
Rice KD, Gangloff AR, Kuo EY, Dener JM, Wang VR, Lum R, Newcomb WS, Havel C, Putnam D, Cregar L, Wong M, Warne RL.
Bioorg Med Chem Lett (2000) 10 : 2357 -2360
PubMed 11055355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 4.24 4.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310289 1 4.42
CHEMBL46809 1 4.41
CHEMBL43463 1 4.36
CHEMBL80210 1 4.30
CHEMBL77911 1 4.25
CHEMBL79545 1 4.16
CHEMBL46120 1 4.14
CHEMBL408300 1 4.14
CHEMBL75749 1 4.11
CHEMBL310290 1 4.08
CHEMBL79822 1 -
CHEMBL78757 1 -
CHEMBL309788 1 -
CHEMBL80149 1 -
CHEMBL77521 1 -
CHEMBL79655 1 -
CHEMBL76733 1 -
CHEMBL306537 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310289 Ki = 38000.0 nM 4.42
CHEMBL46809 Ki = 39000.0 nM 4.41
CHEMBL43463 Ki = 44000.0 nM 4.36
CHEMBL80210 Ki = 50000.0 nM 4.30
CHEMBL77911 Ki = 56000.0 nM 4.25
CHEMBL79545 Ki = 70000.0 nM 4.16
CHEMBL46120 Ki = 73000.0 nM 4.14
CHEMBL408300 Ki = 72000.0 nM 4.14
CHEMBL75749 Ki = 78000.0 nM 4.11
CHEMBL310290 Ki = 84000.0 nM 4.08
CHEMBL79822 Ki = 162000.0 nM -
CHEMBL78757 Ki > 1000000.0 nM -
CHEMBL309788 Ki = 146000.0 nM -
CHEMBL80149 Ki = 273000.0 nM -
CHEMBL77521 Ki = 317000.0 nM -
CHEMBL79655 Ki = 182000.0 nM -
CHEMBL76733 Ki = 237000.0 nM -
CHEMBL306537 Ki = 274000.0 nM -