. Author manuscript; available in PMC: 2019 Oct 11.

Published in final edited form as: J Med Chem. 2019 Mar 27;62(7):3753–3772. doi: 10.1021/acs.jmedchem.9b00351

Table 4.

SFSR of the LHS Moiety of Compound 1^a


Cmpd	LHS	EC₅₀(nM)	pEC₅₀ ± SEM	E_max ± SEM(%)	EC₅₀(nM)	pEC₅₀ ± SEM	E_max ± SEM(%)	Bias for cAMP accumulation
1		0.25	9.61 ± 0.18	61 ±3	110	6.94 ± 0.16	48 ± 3	7.7
26		62	7.21 ± 0.08	67 ± 2	N.A.	N.A.	N.A.	N.C.
27		79	7.10 ± 0.05	69 ± 1	N.A.	N.A.	N.A.	N.C.
28		15	7.84 ± 0.06	82 ± 2	>10,000	<5.00	N.D.	N.C.
29		0.23	9.64 ± 0.05	100 ± 1	22	7.67 ± 0.10	63 ± 2	1.9
30		0.87	9.06 ± 0.09	83 ± 2	690	6.16 ± 0.19	59 ± 4	15
31		260	6.59 ± 0.03	85 ± 1	N.A.	N.A.	N.A.	N.C.
32		1.8	8.76 ± 0.04	104 ± 1	>10,000	<5.00	N.D.	N.C.
33		120	6.91 ± 0.06	83 ± 2	>10,000	<5.00	N.D.	N.C.
34		>10,000	<5.00	N.D.	N.A.	N.A.	N.A.	N.C.
35		160	6.79 ± 0.11	34 ±1	N.A.	N.A.	N.A.	N.C.
36		640	6.19 ± 0.07	26 ± 1	N.A.	N.A.	N.A.	N.C.

EC₅₀ and E_MAX values are the mean of at least three independent experiments performed in triplicate with standard error of the mean (SEM) values. N.A. no activity at maximum concentration tested (10⁻⁴ M), N.D. not determined, N.C. not calculable.