Table 1. In vitro IC₅₀ (nM) values of the peptides against αvβ3, αvβ5, α5β1 and αIIbβ3 integrins determined from competitive ELISAs. The efficacy (in cellulo IC₅₀ in nM) was determined from the competitive cell-adhesion to vitronectin with αvβ5 expressing MDA-MB-231 breast cancer cells and αvβ3, αvβ5 and α5β1 expressing U-87 MG glioblastoma cells. MCF7 breast cancer cells were taken as negative control in the cell-adhesion assay, where the IC₅₀ for all the analogs was in the high μM range (data not shown). n = 5 ± SEM.

Compound	In vitro				In cellulo		αvβ3Xαvβ5 a
	αvβ3	αvβ5	α5β1	αIIbβ3	MDA-MB-231	U-87 MG
6	140 ± 95	516 ± 117	164 ± 134	>105	>105	>105	>105
7	372 ± 52	0.7 ± 0.2	1.3 ± 0.6	>104	4 ± 2	326 ± 97	260.4
9	>105	>104	53 ± 42	>104	>105	>105	>105
10	252 ± 200	>105	>105	>105	>105	>105	>105
11	72 ± 63	1.3 ± 1	62 ± 45	>105	4.2 ± 4	96 ± 77	93.6
9a	169 ± 100	0.5 ± 0.3	23 ± 12	>105	11 ± 9	40 ± 28	84.5
9b	0.2 ± 0.1	1.6 ± 0.3	2 ± 0.4	>105	1 ± 0.1	1.6 ± 0.6	0.32
9c	>105	>104	461 ± 246	>105	>105	>105	>105
9d	584 ± 504	>104	104 ± 95	>105	>105	>105	>105
12	166 ± 98	>104	48 ± 20	>105	>105	>105	>105
Cilen	0.6 ± 0.4	3 ± 2	6 ± 1	>105	1.2 ± 1	3 ± 2	1.8

^aMultiplication of in vitro IC₅₀ against these integrins.