Monovalent (21a) 1.0 1.0 1.0 Divalent (21b) 1.3 1.1 6.7 Tetravalent (21c) 1.9 2.0 63 Octavalent (21d) 5.3 4.4 39 2 Table 2 Multivalent compounds targeted against LecA. values are calculated versus the β monomeric compounds with linkers, unless otherwise stated Comp. Valency HIA (MIC) ELLA (IC50) SPR (Kd) ITC (Kd) Ref. 1 150 50 106 αMeGal μM μM 1 190 94 106 βMeGal μM μM 22 4 Haemolysis 0.7 = 315 Not soluble 109 μM, β —/— 23 12 0.78 = 0.040 = 0.367 = 51 μM, β μM, β μM, β —/— 458 173 24 4 > 2000 3.5 = 18 1.8 = 83 108 μM —/— μM, β μM, β 25 4 > 2000 2.5 = 25 0.3 = 500 108 μM —/— μM, β μM, β 26 6 63 = 159 0.8 = 80 0.14 = 108 μM, β —/— μM, β μM, β 1071 27 4 63 = 159 1.4 = 45 0.33 = 108 μM, β —/— μM, β μM, β 454
Monovalent (21a) 1.0 1.0 1.0 Divalent (21b) 1.3 1.1 6.7 Tetravalent (21c) 1.9 2.0 63 Octavalent (21d) 5.3 4.4 39 2 Table 2 Multivalent compounds targeted against LecA. β values are calculated versus the monomeric compounds with linkers, unless otherwise stated Comp. Valency HIA (MIC) ELLA (IC50) SPR (Kd) ITC (Kd) Ref. αMeGal 1 150 μM 50 μM 106 βMeGal 1 190 μM 94 μM 106 22 4 Haemolysis 0.7 μM, β = 315 Not soluble —/— 109 23 12 0.78 μM, β = 0.040 μM, β = 458 0.367 μM, β = 173 —/— 51 24 4 > 2000 μM —/— 3.5 μM, β = 18 1.8 μM, β = 83 108 25 4 > 2000 μM —/— 2.5 μM, β = 25 0.3 μM, β = 500 108 26 6 63 μM, β = 159 —/— 0.8 μM, β = 80 0.14 μM, β = 1071 108 27 4 63 μM, β = 159 —/— 1.4 μM, β = 45 0.33 μM, β = 454 108
Chem_Soc_Rev_2013_42_4709-4727.docx