Table 1

Affinity and CDR3 sequences of the parental Fab 72 and optimized variants

AntibodyVH CDR3VL CDR3HaptenEquilibrium, KD95% Confidence interval
Fab 72 GSHLY99DFW100bSASHPPNDALAI GTW91D92I93S94LSAGL Ticagrelor 7.4 nM 1.8-21.5 nM 
Fab 152 GSHLYDFWSASHPPNDALAI GTWLYDRAVGL Ticagrelor 43.2 pM 2.8-119.2 pM 
Fab 162 GSFDYYFWSASHPPNDALAI GTWDISLSAGL Ticagrelor 162.5 pM 125.4-206.3 pM 
MEDI2452 GSFDYYFWSASHPPNDALAI GTWLYDRAVGL Ticagrelor 19.6 pM 13.0-28.7 pM 
   TAM 19.7 pM 4.9-44.7 pM 
   TIM ∼20 nM  
AntibodyVH CDR3VL CDR3HaptenEquilibrium, KD95% Confidence interval
Fab 72 GSHLY99DFW100bSASHPPNDALAI GTW91D92I93S94LSAGL Ticagrelor 7.4 nM 1.8-21.5 nM 
Fab 152 GSHLYDFWSASHPPNDALAI GTWLYDRAVGL Ticagrelor 43.2 pM 2.8-119.2 pM 
Fab 162 GSFDYYFWSASHPPNDALAI GTWDISLSAGL Ticagrelor 162.5 pM 125.4-206.3 pM 
MEDI2452 GSFDYYFWSASHPPNDALAI GTWLYDRAVGL Ticagrelor 19.6 pM 13.0-28.7 pM 
   TAM 19.7 pM 4.9-44.7 pM 
   TIM ∼20 nM  

Changes in sequences from Fab 72 are in bold type. Key residues relating to Figure 2 are followed by Kabat numbers in superscript.

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