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. Author manuscript; available in PMC: 2017 Aug 26.
Published in final edited form as: Chemistry. 2016 Jul 26;22(36):12916–12930. doi: 10.1002/chem.201601468

Table 2.

CXCR4 IC50 values (nM) of the evaluated compounds

Complex CXCL12 inhibition
(nM)
Ca2+ flux IC50
CXCR4a (nM)
[Cu1(OAc)]+ 28.0 186.0
[Zn1(OAc)]+ 153.5 2236.0
[Cu2(OAc)]+ 16.8 298.1
[Zn2(OAc)]+ 117.7 642.5
[Cu3(OAc)]+ 12.4 53.5
[Zn3(OAc)]+ 195.0 2793.8
[Cu4(OAc)]+ 26.4 203.5
[Zn4(OAc)]+ 21.0 40.0
[Cu5(OAc)]+ 29.8 155.8
[Zn5(OAc)]+ 14.8 68.5
[Cu6(OAc)]+ 44.5 231.6
[Zn6(OAc)]+ 15.0 71.0
[Cu8(OAc)]+ 9.5 52.8
[Zn8(OAc)]+ 0.6 1.5
[Cu9(OAc)]+ 68.8 884.1
[Zn9(OAc)]+ 129.0 1163.4
AMD3100 11.9 87.6

CXCR4-positive U87 cell line. IC50 is the concentration of the compound required to inhibit 50% of binding of AF647-labeled CXCL12 (CXCL12 inhibition) the CXCL12 (SDF-1) induced Ca2+ signalling.