Antagonist | |||||||
---|---|---|---|---|---|---|---|
Construct | TAK-779 | Teijin Compound 1 | |||||
IC50 | Log IC50 | IC50 | Log IC50 | ||||
nM | M | nM | M | ||||
WT CCR2 (1 nM) | 5.78 | −8.24 ± 0.20 | 370.68 | −6.43 ± 0.17 | |||
W98A2.60 (10 nM) | 142.23 | −6.85 ± 0.33 | 13,995.87 | −4.85 ± 39.64 | |||
Y120A3.32 (10 nM) | 2.29 | −8.64 ± 0.08 | 3.92 | −8.41 ± 0.19 | |||
H121A3.33 (1 nM) | 7.42 | −8.13 ± 0.21 | 20,276.82 | −4.69 ± 2.70 | |||
F125A3.37 (1 nM) | 7.80 | −8.11 ± 0.18 | 152.26 | −6.81 ± 0.11 | |||
I208A5.44 (1 nM) | 4.87 | −8.31 ± 0.15 | 332.66 | −6.48 ± 0.10 | |||
I263A6.55 (1 nM) | 6.26 | −8.20 ± 0.15 | 4808.39 | −5.32 ± 0.36 | |||
E291Q7.39 (100 nM) | 0.69 | −9.16 ± 0.04 | 26.79 | −7.57 ± 0.25 | |||
T292V7.40 (1 nM) | 414.70 | −6.38 ± 1.15 | N.O.A. | N.O.A. |
N.O.A., no observable antagonism (i.e., at ≥1000-fold excess of antagonist, less than 50% inhibition of migration was observed).