TABLE 2

Agonist response to compounds as determined from CRE-SPAP gene transcription in CHO-β₁ and CHO-β₂ cells given as log values and % 10 μM isoprenaline responses in n separate experiments

Agonist responses were also examined in the presence of CGP20712A (β₁AR) or ICI118551 (β₂AR), and where a parallel shift was achieved, a log value for the antagonist is also given. No response was seen for CGP20712A, ICI118551, nor the docking screen compounds 13^a, 14^a, 15^a, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27 (n = 5 for each ligand at each receptor).

Compound	β₁AR						β₂AR						Log(Efficacy Ratio)
Compound	Log	% Isop	n	Log	CGP20712A	n	Log	% Isop	n	Log	ICI118551	n	β₁AR	β₂AR
Literature known reference compounds
Cimaterol	−8.6 ± 0.1	100 ± 9	12	−9.0 ± 0.1		20	−9.7 ± 0.1	98 ± 6	12	−9.7 ± 0.1		23	2.21	2.59
Salbutamol	−6.5 ± 0.2	109 ± 9	7	−9.0 ± 0.2		6	−8.6 ± 0.1	95 ± 6	6	−9.8 ± 0.1		7	1.55	2.39
Salmeterol	−6.8 ± 0.1	110 ± 9	7	−8.9 ± 0.3		4	−10.9 ± 0.2	100 ± 7	8	−9.1 ± 0.0		6	1.02	1.81
Denopamine	−8.1 ± 0.1	101 ± 4	7	−9.2 ± 0.3		4	−6.4 ± 0.1	65 ± 6	7	−9.6 ± 0.1		4	2.13	1.02
CGP 12177	−8.5 ± 0.1	82 ± 7	13	−7.0 ± 0.1		7	−9.7 ± 0.1	37 ± 4	10	−9.6 ± 0.1		14	−0.92	0.16
Compounds chosen from docking calculations
1	−7.5 ± 0.1	80 ± 4	8	−8.6 ± 0.1		7	−8.0 ± 0.1	90 ± 6	7	−9.6 ± 0.1		6	1.2	1.76
2	−7.2 ± 0.1	82 ± 6	7	−8.6 ± 0.2		5	−7.5 ± 0.1	97 ± 4	7	−9.5 ± 0.1		6	1.22	1.64
3	−6.3 ± 0.1	33 ± 6	6				−7.0 ± 0.1	95 ± 8	6	−9.6 ± 0.1		5	1.27	1.39
4	−6.7 ± 0.1	60 ± 6	7				−7.1 ± 0.1	79 ± 4	7	−9.5 ± 0.1		6	1.25	1.24
11^{^a}	−6.6 ± 0.1	113 ± 7	6	−9.4 ± 0.3		3	−6.5 ± 0.1	92 ± 9	6	−9.7 ± 0.2		5	1.35	1.23
5	−7.0 ± 0.2	85 ± 7	6	−9.1 ± 0.3		4	−6.5 ± 0.1	86 ± 11	6	−9.6 ± 0.1		5	1.42	1.19
12^{^a}	−7.3 ± 0.1	78 ± 6	7	−9.3 ± 0.1		5	−7.2 ± 0.1	96 ± 9	6	−9.7 ± 0.1		6	1.10	1.05
6	−6.8 ± 0.1	82 ± 9	6	−9.0 ± 0.2		3	−6.6 ± 0.1	75 ± 8	6	−9.8 ± 0.1		5	0.92	0.89
7	−6.9 ± 0.0	90 ± 5	6	−9.1 ± 0.2		3	−6.6 ± 0.1	86 ± 6	7	−9.6 ± 0.1		6	1.09	0.73
8	10 μM = 21 ± 7		8				−6.2 ± 0.1	35 ± 7	6
9	10 μM = 30 ± 12		7				10 μM = 29 ± 4		7
10	No response		6				10 μM = 50 ± 8		7

Isop, isoprenaline.
↵^a Molecules selected from secondary screen.