Table 1

IC50 values determined by SPR-based and tenase activity assays

Compound IDChemBridge IDIC50 for inhibition of FVIII-membrane binding, µM (mean)IC50 for inhibition of tenase activity, µM (mean)IC50 for inhibition of C2 domain-membrane binding, µM (mean)
A11-8* 5992471 3.3 9.2 3.9 
D7-5 5651006 2.1 26.9 2.4 
H5-8 6844287 2.7 3.5 47 
C11-10 7687521 3.5 4.2 4.6 
C8-4 5898659 9.6 5.6 52.5 
D11-5 5941257 6.7 10.1 22.9 
D6-7 6656941 19.9 59.7 33.7 
C8-5 5740628 10.6 18.5 33.6 
B7-5 5731791 8.1 38.6 20.2 
Compound IDChemBridge IDIC50 for inhibition of FVIII-membrane binding, µM (mean)IC50 for inhibition of tenase activity, µM (mean)IC50 for inhibition of C2 domain-membrane binding, µM (mean)
A11-8* 5992471 3.3 9.2 3.9 
D7-5 5651006 2.1 26.9 2.4 
H5-8 6844287 2.7 3.5 47 
C11-10 7687521 3.5 4.2 4.6 
C8-4 5898659 9.6 5.6 52.5 
D11-5 5941257 6.7 10.1 22.9 
D6-7 6656941 19.9 59.7 33.7 
C8-5 5740628 10.6 18.5 33.6 
B7-5 5731791 8.1 38.6 20.2 
*

All values are averages of at least 2 dose-response curves (for SPR-based methods) and of triplicates (tenase activity assay).

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