TABLE 3

Association and dissociation rate constants of selected AR ligands

CompoundTarget
(h, human; r, rat)
Temp (°C)kon (M−1·min−1)koff (min−1)RT (min)Kinetic KD (nM)aReference
7CCPAhA1AR259.6 × 1061.20.9131(Guo et al., 2014b)
6NECAhA1AR259.0 × 1050.472.1522(Guo et al., 2014b)
35LUF5834hA1AR252.0 × 1080.921.14.6(Guo et al., 2014b)
36CapadenosonhA1AR252.4 × 1070.036281.5(Louvel et al., 2015)
37LUF6976hA1AR253.9 × 1080.871.12.2(Louvel et al., 2014)
38LUF6941hA1AR252.6 × 1060.00761322.9(Louvel et al., 2015)
39ABA-X-BY630hA1ARb372.6 × 1072.00.577(May et al., 2010)
17DPCPXhA1AR251.4 × 1080.214.81.5(Guo et al., 2013)
17DPCPXrA1R259.6 × 1070.04522.20.50(Guo et al., 2017)
10CGS21680hA2AAR255.0 × 1040.0250.0380(Guo et al., 2017)
10CGS21680rA2AAR232.1 × 1070.03330.31.6(Guo et al., 2017)
40LUF6057hA1AR254.8 × 1083.00.36.3(Guo et al., 2013)
6NECAhA2AAR41.9 × 1060.0531928(Guo et al., 2015)
11UK432,097hA2AAR55.0 × 1050.0042508.0(Guo et al., 2012)
41SCH58261hA2AAR256.4 × 1081.50.672.3(Dionisotti et al., 1997)
42ZM241385hA2AAR41.3 × 1080.014710.11(Guo et al., 2014c)
43LUF6632hA2AAR43.4 × 1070.00313230.091(Guo et al., 2014c)
20aMSX-2rA2AAR (brain
striatal membranes)
2314.5 × 1070.28393.521.95(Müller et al., 2000)
6NECAhA2BAR4n.d.2.2010.45n.d.(Hinz et al., 2018)
23MRS1754hA2BAR252.2 × 1070.027371.2(Ji et al., 2001)
44MRE2029-F20hA2BAR41.7 × 1070.031321.8(Baraldi et al., 2004)
45OSIP339391hA2BAR229.5 × 1070.039260.41(Stewart et al., 2004)
24PSB-603hA2BAR2111.4 × 1070.02279440.652(Borrmann et al., 2009)
46PSB-298hA2BAR253.76 × 1070.95331.0525(Bertarelli et al., 2006)
47I-AB-MECAhA3AR376.1 × 1070.042240.69(Gao et al., 2001)
48IB-MECAhA3AR103.5 × 1070.011950.30(Xia et al., 2018)
142-Cl-IB-MECAhA3AR102.4 × 1070.00432310.18(Xia et al., 2018)
49MRS5127hA3AR252.4 × 1080.512.02.1(Auchampach et al., 2010)
16MRS5698hA3AR107.8 × 1065.1 × 10−419610.068(Xia et al., 2018)
31MRE3008-F20hA3AR47.6 × 1070.042240.55(Varani et al., 2000)
50LUF7531 (cmpd 2)hA3AR101.7 × 1080.00363150.021(Xia et al., 2017)
51PSB-11hA3AR252.35 × 1080.20824.800.46(Müller et al., 2002)
  • n.d., no data.

  • a(kinetic) KD = koff/kon.

  • bwhole cells.