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. 2017 Dec 22;61(3):724–733. doi: 10.1021/acs.jmedchem.7b01249

Table 1. Binding Affinity (Kd), Protein Stability Change (ΔTm), and Half-Maximum Inhibitory Concentration (IC50).

      IC50 (μM)b
inhibitor Kd (μM) ΔTm (°C)a Vero E6 HepG2
toremifene 16 –15 0.162 (0.048) 0.026 (0.0013)
benztropine 1300 –6 8.07 (0) 2.82 (0.13)
bepridil 290 –6 5.08 (0.38) 3.21 (0.15)
paroxetine 650 –4 7.45 (0.41) 1.38 (0.076)
sertraline 950 –3 3.13 (0.24) 1.44 (0.057)
a

ΔTm is measured at inhibitor concentration of 500 μM.

b

IC50 values and standard deviations (in parentheses) are adapted from Johansen et al.15