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Assay Detail

CHEMBL1947445

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

Binding
Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry
16
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).
Venkatraj M, Messagie J, Joossens J, Lambeir AM, Haemers A, Van der Veken P, Augustyns K.
Bioorg Med Chem (2012) 20 : 1557 -1568
PubMed 22285569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.25 4.25
Ki 4 6.19 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158405 1 7.00
CHEMBL107955 1 6.31
CHEMBL104937 2 5.25
CHEMBL324168 2 -
CHEMBL1945236 1 -
CHEMBL1945669 1 -
CHEMBL1945756 1 -
CHEMBL1945757 1 -
CHEMBL1945764 1 -
CHEMBL1945765 1 -
CHEMBL1945766 1 -
CHEMBL1945767 1 -
CHEMBL1945918 1 -
CHEMBL112995 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158405 Ki = 100.0 nM 7.00
CHEMBL107955 Ki = 490.0 nM 6.31
CHEMBL104937 Ki = 5640.0 nM 5.25
CHEMBL104937 IC50 = 56000.0 nM 4.25
CHEMBL324168 Ki > 100000.0 nM -
CHEMBL1945236 IC50 > 100000.0 nM -
CHEMBL1945669 IC50 > 125000.0 nM -
CHEMBL1945756 IC50 > 62000.0 nM -
CHEMBL1945757 IC50 > 62000.0 nM -
CHEMBL1945764 IC50 > 62000.0 nM -
CHEMBL1945765 IC50 > 62000.0 nM -
CHEMBL1945766 IC50 > 62000.0 nM -
CHEMBL1945767 IC50 > 62000.0 nM -
CHEMBL1945918 IC50 > 62000.0 nM -
CHEMBL112995 IC50 > 62000.0 nM -
CHEMBL324168 IC50 > 62000.0 nM -