The effect of the N-alkyl moiety on the interaction of pindolol analogues with the two agonist conformations of the human β1-adrenoceptor

Unknown, Conference object English OPEN
Mistry, Shailesh N. ; Baker, Jillian G. (2016)
  • References (1)

    Log KD n -8.67±0.04 7 -9.40±0.04 10 -7.70±0.04 6 -7.78±0.05 6 -8.77±0.04 6 -8.37±0.03 6 -8.26±0.04 5 -9.82±0.04 10 -8.74±0.04 -8.40±0.06 -8.30±0.06 -9.01±0.05 -7.64±0.03 -9.54±0.05 No binding No binding 6 6 6 9 6 6 4 4 Log EC501 Log EC502 % site 1 % isop max n -8.86±0.18 -6.32±0.32 51.6±3.6 74.8±10.2 6 -9.16±0.11 -6.51±0.13 55.8±4.3 77.0±5.4 8 -8.16±0.08 -5.84±0.12 56.5±7.5 69.6±4.2 6 -8.21±0.09 -5.69±0.19 43.2±6.5 64.6±5.3 8 -8.96±0.13 -6.39±0.20 50.0±3.5 67.2±7.3 9 -8.50±0.10 -5.92±0.09 48.5±3.5 70.2±5.9 8 -8.41±0.07 -5.88±0.08 44.6±3.4 71.5±8.1 7 -9.19±0.14 -6.70±0.34 65.0±4.5 83.2±6.5 8 -8.84±0.10 -6.25±0.10 42.7±3.2 -8.93±0.09 -6.35±0.12 58.3±4.1 -8.45±0.05 -6.01±0.08 41.8±3.0 -9.09±0.08 -6.38±0.30 58.2±7.1 -8.05±0.06 -6.01±0.08 53.4±5.8 72.7±5.1 73.9±7.1 76.1±7.7 81.1±9.2 66.7±9.7 -9.62±0.11 -6.99±0.21 64.2±6.4 72.7±6.9 No response No response 8 7 8 6 6 7 8 8

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