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. 2023 Mar 21;66(7):5208–5222. doi: 10.1021/acs.jmedchem.3c00151

Table 2. Binding Affinities (pKi) of CXCL12, AMD3100, and IT1t as Calculated from Cheng–Prusoff Analysis of the Data Displayed in Figure 4.

  IT1t
AMD3100
CXCL12
example pIC50 pKi pIC50 pKi % max. inhibition of AMD3100a pIC50 pKi
10 7.70 ± 0.13 (4) 8.04 ± 0.11 (4) 6.47 ± 0.20 (4) N.D 75.26 ± 7.08 N.D N.D
11 8.18 ± 0.12 (4) 8.50 ± 0.07 (4) 7.16 ± 0.11 (4) 7.45 ± 0.07 (4) 95.20 ± 9.60 N.D N.D
18b 7.57 ± 0.36 (3) 8.59 ± 0.06 (3) 6.82 ± 0.66 (3) 7.29 ± 0.06 (3) 96.25 ± 3.82 N.D N.D
CXCL12AF-647   8.04 ± 0.01 (5)   7.00 ± 0.04 (5)     7.97 ± 0.07 (5)
a

Maximum inhibition of AMD3100 in respect to IT1t, calculated following baseline removal of BRET ratios measured at 10–11 M. Data were then normalized as a percentage of maximum inhibition seen at 10–5 M IT1t (100%). All values are expressed as mean ± S.E.M. Number of experiments are shown in parenthesis.