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Assay Detail

CHEMBL1005173

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

Binding
Inhibition of human factor 12a
27
Total Activities
27
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

Coagulation factor XII (CHEMBL2821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
Robert S, Bertolla C, Masereel B, Dogné JM, Pochet L.
J Med Chem (2008) 51 : 3077 -3080
PubMed 18459730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 4.83 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521527 1 6.75
CHEMBL521526 1 5.37
CHEMBL493601 1 5.36
CHEMBL444181 1 5.08
CHEMBL494978 1 5.01
CHEMBL494808 1 5.00
CHEMBL495154 1 5.00
CHEMBL523874 1 4.82
CHEMBL274376 1 4.77
CHEMBL494799 1 4.72
CHEMBL522532 1 4.70
CHEMBL494632 1 4.66
CHEMBL495466 1 4.64
CHEMBL494633 1 4.62
CHEMBL495153 1 4.60
CHEMBL522376 1 4.54
CHEMBL495225 1 4.52
CHEMBL494798 1 4.51
CHEMBL495155 1 4.50
CHEMBL502858 1 4.50
CHEMBL495465 1 4.48
CHEMBL494800 1 4.47
CHEMBL494795 1 4.38
CHEMBL493602 1 -
CHEMBL493615 1 -
CHEMBL495467 1 -
CHEMBL13357 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521527 IC50 = 180.0 nM 6.75
CHEMBL521526 IC50 = 4300.0 nM 5.37
CHEMBL493601 IC50 = 4400.0 nM 5.36
CHEMBL444181 IC50 = 8300.0 nM 5.08
CHEMBL494978 IC50 = 9800.0 nM 5.01
CHEMBL494808 IC50 = 10000.0 nM 5.00
CHEMBL495154 IC50 = 10000.0 nM 5.00
CHEMBL523874 IC50 = 15000.0 nM 4.82
CHEMBL274376 IC50 = 17000.0 nM 4.77
CHEMBL494799 IC50 = 19000.0 nM 4.72
CHEMBL522532 IC50 = 20000.0 nM 4.70
CHEMBL494632 IC50 = 22000.0 nM 4.66
CHEMBL495466 IC50 = 23000.0 nM 4.64
CHEMBL494633 IC50 = 24000.0 nM 4.62
CHEMBL495153 IC50 = 25000.0 nM 4.60
CHEMBL522376 IC50 = 29000.0 nM 4.54
CHEMBL495225 IC50 = 30000.0 nM 4.52
CHEMBL494798 IC50 = 31000.0 nM 4.51
CHEMBL495155 IC50 = 32000.0 nM 4.50
CHEMBL502858 IC50 = 32000.0 nM 4.50
CHEMBL495465 IC50 = 33000.0 nM 4.48
CHEMBL494800 IC50 = 34000.0 nM 4.47
CHEMBL494795 IC50 = 42000.0 nM 4.38
CHEMBL493602 IC50 > 50000.0 nM -
CHEMBL493615 IC50 > 50000.0 nM -
CHEMBL495467 IC50 > 50000.0 nM -
CHEMBL13357 IC50 > 50000.0 nM -