TABLE 1.

Binding parameters of orthosteric ligands and allosteric modulators

K_i, K_B, and α values are shown with corresponding 95% confidence intervals in parentheses. For the first row, [³H]CP55940 and for the second row [³H]SR141716A are used as the orthosteric tracers. Three independent experiments, each done in duplicate, were used in each case.

	CP55940	SR141716A	LDK1285		LDK1288		LDK1305		PSNCBAM1
	Ki	Ki	KB	α	KB	α	KB	α	KB	α
[3H]CP55940	nM	nM	nM	11.5	nM	5.3	nM	4.3	nM	2.7
	1.24	ND	198		62.5		20.0		41.4
	(0.62–2.48)		(141–277)	(7.7–17.2)	(41.6–94.1)	(3.9–7.2)	(13.5–29.5)	(3.4–5.6)	(18.8–91.1)	(2.1–3.5)
[3H]SR141716A	ND	2.13	473	0.1	224	0.1	115	0.3	156	0.1
		(1.37–3.32)	(160–1350)	(0.0–0.3)	(64.4–722)	(0.0–0.3)	(29.9–454)	(0.1–0.4)	(14.2–983)	(0.0–0.4)

K_i, equilibrium dissociation constant of orthosteric ligand; K_B, equilibrium dissociation constant of allosteric modulator; α, cooperativity factor between orthosteric and allosteric ligand binding; ND, not done.