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Assay Detail

CHEMBL718140

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Binding
compound was tested for inhibitory activity against Matriptase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Suppressor of tumorigenicity 14 protein (CHEMBL3018)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.
Enyedy IJ, Lee SL, Kuo AH, Dickson RB, Lin CY, Wang S.
J Med Chem (2001) 44 : 1349 -1355
PubMed 11311057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.17 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26370 1 6.72
CHEMBL26856 1 6.68
CHEMBL30044 DIBROMPROPAMIDINE 2.0 1 6.27
CHEMBL25105 HEXAMIDINE 2.0 1 6.03
CHEMBL55 PENTAMIDINE 4.0 1 5.94
CHEMBL27421 1 5.35
CHEMBL285114 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26370 Ki = 191.0 nM 6.72
CHEMBL26856 Ki = 208.0 nM 6.68
CHEMBL30044 DIBROMPROPAMIDINE Ki = 535.0 nM 6.27
CHEMBL25105 HEXAMIDINE Ki = 924.0 nM 6.03
CHEMBL55 PENTAMIDINE Ki = 1160.0 nM 5.94
CHEMBL27421 Ki = 4500.0 nM 5.35
CHEMBL285114 Ki > 10000.0 nM -