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. Author manuscript; available in PMC: 2024 Jun 21.

Published in final edited form as: ACS Chem Neurosci. 2024 Jun 7;15(12):2396–2407. doi: 10.1021/acschemneuro.4c00086

Table 2.

Northern Ring SAR


Cmpd No.	Aryl	% Inhibition at 10 μM^b					D_4.4 IC₅₀ (nM)^a	D_4.4 K_i(nM)^b
Cmpd No.	Aryl	D_4.4	D_2S	D_2L	D₃	D₁	D_4.4 IC₅₀ (nM)^a	D_4.4 K_i(nM)^b
5		94%	25%	24%	27%	35%	200	56
17		93%	11%	26%	34%	24%	77	21
18		42%	-	-	-	-	-	-
19		92%	14%	23%	30%	21%	82	23
20		95%	12%	18%	14%	16%	84	23
21		94%	17%	29%	40%	24%	78	22
22		92%	22%	38%	31%	19%	95	26
23		78%	-	-	-	-	-	-
24		63%	-	-	-	-	-	-
25		66%	-	-	-	-	-	-
26		14%	-	-	-	-	-	-
27		95%	21%	34%	36%	32%	28	7.6
28		49%	-	-	-	-	-	-
29		99%	5%	20%	13%	27%	62	17
30		95%	17%	35%	23%	10%	790	220
31		93%	22%	26%	35%	21%	260	71
32		92%	18%	18%	12%	10%	490	140
33		93%	0%	−7%	11%	9%	210	59
34^a		94%	17%	50%	49%	47%	120	33

^a

Structure for this compound is a sulfonamide bound to the azetidine nitrogen of the spirocycle.

^b

Values were obtained from Eurofins Discovery. See Supporting Information for more details.