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. 2015 Mar 30;6(5):502–506. doi: 10.1021/ml5004298

Table 1. Comparison of the Probes’ Affinity to α1-ARs.

  Kia(nM)
IC50 (nM)
compd α1A α1B α1D α1A α1B α1D
phentolamine 0.6 4.8 7.6 1.1 10.8 12.5
1a 2.1 NAc NAc 3.9 <5b <5b
1b 1.3 NAc NAc 2.5 <5b <5b
1c 0.3 0.1 0.4 0.6 1.2 2.2
1d 4.7 7.3 20.7 8.8 16.3 34.0
1e 29.9 29.9 27.5 52.4 52.4 45.2
a

Ki was calculated from IC50 using the Cheng–Prusoff equation.

b

Data was estimated from the unclassical binding-competitive curve.

c

Not available.