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. Author manuscript; available in PMC: 2015 Jan 3.

Published in final edited form as: Expert Opin Investig Drugs. 2013 Dec 13;23(2):227–241. doi: 10.1517/13543784.2014.856879

Table 3.

In vitro binding affinity and functional activity data of dicarba-cyclic ligands.


Compound number	GPI		MVD		GPI/MVD	OR binding affinity			Binding ratio

	IC₅₀(nM)	K_e (nM)	IC₅₀ (nM)	K_e (nM)	IC₅₀ ratio	K_i^μ (nM)	K_i^δ (nM)	K_i^κ (nM)	K_i^μ/K_i^δ/K_i^κ
36	0.401	–	0.851	–	1/2	0.281	0.92	9.36	1/3/12
37	1.34	–	4.51	–	1/3	0.332	1.53	15.2	1/5/14
38	1.05	–	0.740	–	1.4/1	1.04	2.24	11.3	1/2/11
39	0.161	–	0.191	–	1/1.2	0.528	0.49	12.8	1/1/24
40	0.407	–	0.0444	–	9/1	0.438	0.29	4.97	1/1/11
41	0.509	–	0.0655	–	8/1	1.54	1.20	15.8	1/1/10
42	–	32.2	PA (e = 0.38)	–	–	23.5	86.3	266	1/4/11
43	–	44.3	239	–	–	16.7	27.0	> 500	1/2/> 30
44	–	41.7	7500	–	–	8.95	39.2	> 500	1/4/> 56
45	–	32.4	PA	–	–	7.44	7.67	185	1/1/25
46	–	157	PA (e = 0.33)	–	–	323	35.3	635	1/0.1/2
47	–	25.7	9.91	147	–	18.3	18.7	302	1/1/17
48	–	–	–	–	–	0.016	1.8	2.5	1/112/156