Cu(II)-Bipyridine | Zn(II)-Bipyridine | Cu(II)-Phenanthroline | ||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
EC50 | Kd | n | Fdec. | EC50 | Kd | n | Fdec. | EC50 | Kd | n | Fdec. | |||||||||||
μM | -fold | μM | -fold | nM | -fold | |||||||||||||||||
III:05 | G128H | -4.7 ± 0.11 | 22 | 18 | 1.0 | -4.3 ± 0.08 | 53 | 15 | 1.0 | -4.7 ± 0.05 | 21 | 8 | 1.0 | |||||||||
Background | ||||||||||||||||||||||
III:08 | F131A | -2.8 ± 0.09 | 1415a | 4 | 64 | -3.0 ± 0.15 | 971a | 6 | 18 | -3.0 ± 0.13 | 989a | 6 | 47 | |||||||||
IV:20 | D186N | -3.1 ± 0.43 | 885a | 8 | 40 | -2.9 ± 0.31 | 1240a | 4 | 24 | -3.6 ± 0.14 | 241a | 4 | 12 | |||||||||
V:01; V:05 | R208A;R212A | -4.9 ± 0.04 | 12 | 4 | 0.55 | -4.5 ± 0.08 | 29 | 3 | 0.55 | -5.1 ± 0.15 | 7.9 | 3 | 0.38 | |||||||||
VI:13 | W268A | -4.3 ± 0.08 | 50 | 5 | 2.3 | -3.7 ± 0.24 | 190 | 4 | 3.6 | -4.5 ± 0.08 | 33 | 6 | 1.6 | |||||||||
VI:16 | Y271A | -3.1 ± 0.21 | 812a | 4 | 37 | -2.9 ± 0.27 | 1278a | 3 | 24 | -3.4 ± 0.02 | 433a | 3 | 21 | |||||||||
VI:23 | D278N | -4.3 ± 0.12 | 55 | 6 | 2.5 | -3.7 ± 0.16 | 212 | 3 | 4.0 | -4.5 ± 0.04 | 35 | 4 | 1.7 | |||||||||
VII:02 | K300A | -4.7 ± 0.09 | 20 | 4 | 0.90 | -4.3 ± 0.07 | 45 | 3 | 0.86 | -5.1 ± 0.07 | 7.8 | 3 | 0.37 | |||||||||
VII:10 | Y308A | -3.2 ± 0.45 | 651a | 3 | 29 | -3.2 ± 0.70 | 568a | 3 | 11 | -3.4 ± 0.07 | 400a | 3 | 19 |
Fdec, decrease in potency for each ligand on a given mutation compared with His III:05-CXCR3 (background).
↵ a The EC50 was estimated by a nonlinear regression using the sigmoidal dose-response algorithm in GraphPad Prism with a constant Hill coefficient of 1.5 corresponding to the Hill coefficient of the metal ion chelator complexes on His III:05 CXCR3.