Skip to main content
. Author manuscript; available in PMC: 2015 Sep 15.
Published in final edited form as: Bioorg Med Chem Lett. 2014 Aug 8;24(18):4466–4471. doi: 10.1016/j.bmcl.2014.07.091

Table 1.

Affinity of Pyridazinoindoles

graphic file with name nihms-620016-f0002.jpg
Compd R C6 Glioma Ki (pM)b Heart Ki (pM)b Kidney Ki (pM)b
3a Ph 1.23 ± 0.08 0.762 ± 0.15 0.596 ± 0.04
9 2-fluorophenyl 0.422 ± 0.06 0.591 ± 0.10 1.18 ± 0.04
10 3-fluorophenyl 0.280 ± 0.07 0.180 ± 0.02 0.212 ± 0.02
11 3-nitrophenyl 0.889 ± 0.2 1.18 ± 0.09 0.678 ± 0.2
12 4-fluorophenyl 0.671 ± 0.2; 3020 ± 1007d 0.877 ± 0.03 0.459 ± 0.03; 969 ± 752d
13 2-pyridyl 2409 ± 795.4 4936 ± 662.3 6796 ± 830.9
14c 3-fluoro-2-pyridyl |1.19 ± 0.05; 1770 ± 232.6d 3.21 ± 0.4 2.21 ± 0.4
15 3-chloro-2-pyridyl 2.34 ± 0.4 0.676 ± 0.08 0.495 ± 0.03
16 3-bromo-2-pyridyl 1.48 ± 0.2 0.281 ± 0.01 0.965 ± 0.02
a

SSR180575.

b

Ki ± S.E.M. versus [3H]PK11195.

c

Ki versus [3H]flunitrazepam in rat brain lysate >10 μM.

d

Mixed affinity binding. All lysates procured from athymic nude rats. All experiments performed in triplicate.