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Assay Detail

CHEMBL4426075

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

Binding
Binding affinity to human plasmin assessed as slow binding constant in presence of Mes-DArg-Phe-Arg-AMC after 20 mins by Dixon plot analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Plasminogen (CHEMBL1801)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Hinkes S, Wuttke A, Saupe SM, Ivanova T, Wagner S, Knörlein A, Heine A, Klebe G, Steinmetzer T.
J Med Chem (2016) 59 : 6370 -6386
PubMed 27280436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 9.38 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4458743 1 9.82
CHEMBL4454130 1 9.38
CHEMBL4553652 1 9.37
CHEMBL4560508 1 9.27
CHEMBL4515955 1 9.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4458743 Ki = 0.15 nM 9.82
CHEMBL4454130 Ki = 0.42 nM 9.38
CHEMBL4553652 Ki = 0.43 nM 9.37
CHEMBL4560508 Ki = 0.54 nM 9.27
CHEMBL4515955 Ki = 0.85 nM 9.07