The Discovery of UK-390957: the Challenge of Targeting a Short Half-life, Rapid T SSRI - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 149

10 H CONH 2 H 2 170 410 55 3.9 2.3
11 H CONHMe H 3 450 440 41 4.1 2.8
12 H CONMe 2 H 9 270 270 32 3.8 -
13 H CN H 3 100 3200 36 4.8 3.4
14 H SO 2 NH 2 H 1 90 770 81 3.5 2.3
15 H SO 2 NHMe H 5 270 1250 67 4.1 2.8
16 H SO 2 NMe 2 H 70 1500 2700 58 4.5 3.1
17 H NHSO 2 Me H 3 55 60 67 4.2 2.2
18 H 1,2,4-triazol-1-yl H 4 250 760 43 4.4 2.9
19 H H CO 2 H 60 16700 20300 49 2.8 -
20 H H CONH 2 13 1300 1100 55 3.9 -
21 H H CONHMe 25 3300 5000 41 4.1 -
22 H H CONMe 2 7 920 11500 32 3.8 -
23 H H SO 2 NH 2 6 2500 2100 81 3.5 -
24 H NHSO 2 Me CONH 2 24 3600 2100 110 2.6 -
a The inhibitory potency at human serotonin, dopamine and noradrenaline transporters was quantified through measurement of a compound's ability to inhibit
transport and subsequent intracellular accumulation of radiolabelled ligand in an in vitro radiometric assay using HEK-293 cells stably expressing the appropriate
transporters. All assay determinations are Zn ¼ 2.