TABLE 1

Autoradiographic Characteristics and Ki and Kd Values of THK Compounds

THK no.Autoradiography (tau/Aβ)Ki (nM)Kd (nM)
523++/−183
5377++/−51.3
5378+/+87.2
5140++/+54.8
5035−/−98.4
5156−/−> 1,000
5107−/−142
5116−/−106
5117+++/−27.411.5
5105+++/+10.14.40
5125+/−28.010.2
5151+++/−29.17.07
5129++/+17.53.14
5307+/−83.55.60
5287++/−26.02.60
  • Symbols indicate results of binding intensities semiquantitatively analyzed by ARG-based binding assay. − indicates no binding of compound to tau or Aβ, + corresponds to weak binding, ++ corresponds to moderate binding, and +++ corresponds to strong binding.