TABLE 2

Ligand potencies at hC5a and hC5L2 receptor as measured by radioligand binding with [125I]hC5a


Ligand

Recombinantly Expressed Receptor*
hC5aR
hC5L2R
hC5a** 0.05 ± 0.01 nM 0.85 ± 0.07 nM
hC5a desArg** 14.1 ± 1.7 nM 16.2 ± 3.0 nM
NDT 9513727
11.6 ± 5.3 nM
>10 μM
  • * The CHO cell expression system was used for all examples except NDT 9513727 activity at the hC5aR, which used baculovirus-expressed C5aR. All values shown are IC50 values

  • ** Synthesized and purified using His-tag methodologies (see Materials and Methods)