Figure 2: Different mechanisms of C5aR antagonism by 3D53, W54011 and JJ47 against human C5a on human monocyte-derived macrophages. | Scientific Reports

Figure 2: Different mechanisms of C5aR antagonism by 3D53, W54011 and JJ47 against human C5a on human monocyte-derived macrophages.

From: Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists

Figure 2

Top row: Binding affinities of (A) 3D53, (B) W54011 and (C) JJ47 measured by displacement of [125I]-C5a (25 pM) from HMDM. Middle row: Concentration dependent responses to C5a following treatment with antagonist (D) 3D53, (E) W54011 and (F) JJ47 at various concentrations (0 nM, ●; 3 nM, ■; 10 nM, ▲; 30 nM, ◆; 100 nM, 300 nM, ▼; 1000 nM, ★) with C5a (300 nM) as 100% response on human macrophages in a calcium release assay. Bottom row: Schild plots for antagonists (G) 3D53, (H) W54011 and (I) JJ47 against rhC5a. Calculated pA2 values are 8.3 (3D53), 8.6 (W54011) and 8.3 (JJ47). Error bars are means ± SEM of three independent experiments (n = 3).

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