Table 2.

Human D₂-like receptor binding data on full-length analogues^a

Compd	Series	Ar	A	B	C	Linker	cLogPb	PSAc	D2LR	D3R	D4.4R	D2R/D3R
									Ki ± S.E.M. (nM)
18	a		H	OMe	Cl		5.53	56.84	27.8±6.71	0.341±0.031	1050±279	82
19	a		H	OMe	Cl		4.93	77.07	11400±3270	6.84±1.18	13900±1350	1700
20	a		H	OMe	Cl		5.50	54.04	137±9.00	3.19±0.268	714±293	43
21	a		H	OMe	Cl		4.91	74.27	1620±339	36.1±5.00	5290±319	45
22	b		Cl	H	H		5.76	47.61	5.50±0.805	0.142±0.025	334±113	39
23	b		Cl	H	H		5.17	67.84	151±25.4	0.362±0.047	5520±1660	417
24	b		Cl	H	H		5.74	44.81	6.34±0.959	0.153±0.005	356±64.4	41
25	b		Cl	H	H		5.14	65.04	164±32.4	0.985±0.105	2380±110	166
26	b		Cl	H	H		5.52	51.18	5.64±0.98	0.331±0.085	819±175	17
27	b		Cl	H	H		4.93	71.41	193±40.5	4.23±0.84	>10000	46
28	b		Cl	H	H		5.43	51.18	4.65±1.24	0.941±0.13	143±3.18	5
29	b		Cl	H	H		5.38	59.97	12.5±1.07	1.14±0.17	500±30.9	11
30	b		Cl	H	H		4.39	59.97	12.2±2.58	0.621±0.096	529±42.3	20
31	b		Cl	H	H		3.79	80.2	150±13.1	11.2±2.66	1960±344	13
35	b		Cl	H	H		4.31	59.97	16.1±1.2	1.28±0.22	503±157	13
40	b		Cl	H	H		5.05	67.84	6.83±0.53	0.200±0.018	305±70.5	34

^aBinding inhibition values determined using HEK 293 cells transfected with hD_2LR, hD₃R or hD_4.4 and [³H]N-methylspiperone radioligand as described.⁵⁹

^bPartition coefficients (clogP) were calculated using ChemDraw Professional Ultra 15.0.

^cCalculated according to ref. 41.