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Assay Detail

CHEMBL811973

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

Binding
Inhibition of thrombin in human mast cells
15
Total Activities
15
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

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
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 15 4.35 4.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43938 1 4.68
CHEMBL295450 1 4.50
CHEMBL42899 1 4.38
CHEMBL297220 1 4.38
CHEMBL295007 1 4.28
CHEMBL298256 1 4.22
CHEMBL38054 1 4.03
CHEMBL297408 1 -
CHEMBL40491 1 -
CHEMBL42364 1 -
CHEMBL42898 1 -
CHEMBL42037 1 -
CHEMBL289918 1 -
CHEMBL406192 1 -
CHEMBL296733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43938 Ki = 20800.0 nM 4.68
CHEMBL295450 Ki = 31900.0 nM 4.50
CHEMBL42899 Ki = 41200.0 nM 4.38
CHEMBL297220 Ki = 42200.0 nM 4.38
CHEMBL295007 Ki = 52900.0 nM 4.28
CHEMBL298256 Ki = 59500.0 nM 4.22
CHEMBL38054 Ki = 94400.0 nM 4.03
CHEMBL297408 Ki = 386000.0 nM -
CHEMBL40491 Ki = 111000.0 nM -
CHEMBL42364 Ki = 561000.0 nM -
CHEMBL42898 Ki = 102000.0 nM -
CHEMBL42037 Ki > 1000000.0 nM -
CHEMBL289918 Ki > 1000000.0 nM -
CHEMBL406192 Ki = 423000.0 nM -
CHEMBL296733 Ki > 1000000.0 nM -