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Assay Detail

CHEMBL3767388

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

Binding
Inhibition of human factor 12a using S-2302 as substrate assessed as para-nitroaniline release preincubated for 10 mins followed by substrate addition measured after 30 mins by HPLC-UV analysis
6
Total Activities
6
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

Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors.
Bouckaert C, Serra S, Rondelet G, Dolušić E, Wouters J, Dogné JM, Frédérick R, Pochet L.
Eur J Med Chem (2016) 110 : 181 -194
PubMed 26827162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.87 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765536 1 5.30
CHEMBL3763881 1 5.16
CHEMBL3763678 1 5.10
CHEMBL493601 1 4.80
CHEMBL3764790 1 4.47
CHEMBL3763449 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765536 IC50 = 5000.0 nM 5.30
CHEMBL3763881 IC50 = 7000.0 nM 5.16
CHEMBL3763678 IC50 = 8000.0 nM 5.10
CHEMBL493601 IC50 = 16000.0 nM 4.80
CHEMBL3764790 IC50 = 34000.0 nM 4.47
CHEMBL3763449 IC50 = 41000.0 nM 4.39