. 2016 Jun 3;6:27147. doi: 10.1038/srep27147

Table 2. Binding of MK-1064 for OX₁R and OX₂R across species relative to other 2-SORAs and MK-6096 and hOX₂R binding kinetics.

	2-SORAs				DORA
	MK-1064	2-SORA-18	MK-3697	2-SORA-7	MK-6096
OX₁R affinity (K_i in nM)
Mouse	1159	98	3951	1693	2.9
Rat	1069	94	2388	2613	2.5
Rabbit	2438	241	4740	4394	2.6
Dog	1300	86	3100	1800	2.7
Rhesus	815	132	2176	1336	12.5
Human	1500	100	3500	2800	2.5
OX₂R affinity (K_i in nM) [ fold OX₂R selectivity]
Mouse	1.02	0.15	1.47	0.83	0.56
Mouse	[1136]	[653]	[2688]	[2040]	[5.2]
Rat	0.83	0.18	1.93	0.22	0.22
Rat	[1288]	[522]	[1237]	[11877]	[11.4]
Rabbit	0.51	0.10	1.01	0.44	0.28
Rabbit	[4780]	[2410]	[4693]	[9986]	[9.3]
Dog	0.78	0.11	1.10	0.63	0.36
Dog	[1667]	[782]	[2818]	[2857]	[7.5]
Rhesus	0.62	0.11	1.14	0.67	0.44
Rhesus	[1315]	[1200]	[1909]	[1994]	[28.4]
Human	0.52	0.10	0.97	0.47	0.31
Human	[2885]	[1000]	[3608]	[5957]	[8.1]
hOX₂R binding kinetics
K_d (nM)	0.51	ND	1.16	ND	0.34
T_1/2ON (min)	21.1	ND	24.3	ND	62.9
K_ON (min⁻¹)	1.19 × 10⁷		4.69 × 10⁶		9.19 × 10⁶
T_1/2OFF (min)	110	ND	54.4	ND	118.3
K_OFF (mol⁻¹min⁻¹)	6.97 × 10⁻³		1.30 × 10⁻²		1.88 × 10⁻²

ND, not determined.

Table 2. Binding of MK-1064 for OX1R and OX2R across species relative to other 2-SORAs and MK-6096 and hOX2R binding kinetics.