Skip to main content
. Author manuscript; available in PMC: 2018 Feb 1.
Published in final edited form as: Drug Dev Res. 2016 Nov 18;78(1):49–62. doi: 10.1002/ddr.21370

Table 1.

Activity of 4-benzyl-5-substituted pyridazinones 4a-f in human neutrophils and FPR-transfected HL60 cell

graphic file with name nihms-824647-f0004.jpg
Compd R5 OCH3 Ca2+ flux
human neutrophils FPR1-HL60 FPR2-HL60 FPR3-HL60
EC50 (μM) and efficacy (%)[a]
4a CH3 m 0.006 ± 0.002 (150) 0.019 ± 0.005 (85) 0.043 ± 0.016 (80) 0.040 ± 0.011 (165)
4b CH3 p 0.27 ± 0.025 (140) 0.9 ± 0.033 (60) 0.013 ± 0.003 (95) 0.13 ± 0.032 (100)
4c C2H5 m 1.2 ± 0.3 (100) 3.2 ± 0.6 (120) 1.9 ± 0.41 (100) 4.1 ± 1.7 (100)
4d C3H5 m 3.2 ± 1.2 (70) 2.2 ± 0.5 (115) 4.6 ± 1.3 (90) 3.4 ± 0.76 (65)
4e C4H9 m 2.7 ± 0.7 (25) N.A.[b] 15.7 ± 4.2 (90) N.A.
4f C6H5 m 5.4 ± 0.26 (100) 2.2 ± 0.62 (160) N.A. N.A.
[a]

EC50 values represent the average of means from three independent experiments and were determined by nonlinear regression analysis of the concentration-response curves (5-6 points) generated using GraphPad Prism 5 with 95% confidential interval (p < 0.05). Efficacy is expressed as % of the response induced by 5 nM fMLF (FPR1), 5 nM WKYMVm (FPR2), or 10 nM WKYMVM (FPR3).

[b]

N.A., no activity (no response was observed during the first 2 min after addition of compounds under investigation) considering the limits of efficacy > 20% and EC50 < 50 μM.