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Table 1 Binding affinity of the investigated azinesulfonamides 16 for 5-HT1A, 5-HT6, 5-HT7, and D2 receptors

From: Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands

Compound Ki (nM)a
Azinyl n R 5-HT1A 5-HT6 5-HT7 D2
1 3-isoquinolinyl 2 H 304 1352 245 565
2 3-isoquinolinyl 2 3-Cl 38 436 49 47
3 b 3-isoquinolinyl 2 2,3-diCl 34 454 56 17
4 3-isoquinolinyl 2 2,3-diMe 73 916 85 23
5 b 7-quinolinyl 2 2,3-diCl 17 301 31 11
6 b 7-quinolinyl 1 2,3-diCl 14 257 12 16
Aripiprazole 5.6 90 26 0.8
  1. a Mean Ki values (SEM ± 23%) based on three independent binding experiments
  2. b Data taken from Ref. [6]