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Assay Detail

CHEMBL870372

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

Binding
Inhibition of human thrombin activity
24
Total Activities
23
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

Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.
De Nanteuil G, Gloanec P, Béguin S, Giesen PL, Hemker HC, Mennecier P, Rupin A, Verbeuren TJ.
J Med Chem (2006) 49 : 5047 -5050
PubMed 16913694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.81 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215639 1 6.11
CHEMBL211973 1 5.90
CHEMBL378083 1 5.36
CHEMBL214264 1 5.00
CHEMBL212789 1 4.88
CHEMBL379430 1 4.48
CHEMBL215295 1 4.33
CHEMBL215556 1 4.07
CHEMBL448732 1 4.00
CHEMBL214356 1 4.00
CHEMBL214309 1 -
CHEMBL212786 1 -
CHEMBL425613 1 -
CHEMBL424882 1 -
CHEMBL215357 1 -
CHEMBL213774 1 -
CHEMBL212971 1 -
CHEMBL215870 2 -
CHEMBL424901 1 -
CHEMBL426333 1 -
CHEMBL215801 1 -
CHEMBL213120 1 -
CHEMBL380157 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215639 IC50 = 770.0 nM 6.11
CHEMBL211973 IC50 = 1250.0 nM 5.90
CHEMBL378083 IC50 = 4400.0 nM 5.36
CHEMBL214264 IC50 = 10050.0 nM 5.00
CHEMBL212789 IC50 = 13340.0 nM 4.88
CHEMBL379430 IC50 = 33000.0 nM 4.48
CHEMBL215295 IC50 = 47000.0 nM 4.33
CHEMBL215556 IC50 = 85000.0 nM 4.07
CHEMBL214356 IC50 = 100000.0 nM 4.00
CHEMBL448732 IC50 = 100000.0 nM 4.00
CHEMBL214309 IC50 > 33000.0 nM -
CHEMBL212786 IC50 - -
CHEMBL212971 IC50 = 300000.0 nM -
CHEMBL425613 IC50 > 33000.0 nM -
CHEMBL424882 IC50 > 300000.0 nM -
CHEMBL215357 IC50 > 300000.0 nM -
CHEMBL213774 IC50 > 300000.0 nM -
CHEMBL426333 IC50 > 300000.0 nM -
CHEMBL213120 IC50 = 300000.0 nM -
CHEMBL215870 IC50 = 300000.0 nM -
CHEMBL215870 IC50 = 300000.0 nM -
CHEMBL424901 IC50 > 33000.0 nM -
CHEMBL380157 IC50 > 33000.0 nM -
CHEMBL215801 IC50 > 300000.0 nM -