Binding Assay | IC50 (nM) or % Inhibition | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Cmpd 1
|
Cmpd 2
|
Cmpd 3
|
Cmpd 4
|
TR14035
|
BIO7662
| ||||||
α4β7 (RPMI-8866 cells) | |||||||||||
125I-MAdCAM-Ig/Mn2+ | 1.1 | 12.0 | 670 | 0% Inh @ 100 μM | 0.75 | 3,300 | |||||
125I-Cmpd 1/Mn2+ | 0.4 | 65.0 | 960.0 | 0% Inh @ 1 mM | 4.0 | 29% Inh @ 100 nM | |||||
α4β1 (Jurkat cells) | |||||||||||
125I-VCAM-Ig/Mn2+ | 0.10 | 0.08 | 0.5 | 28,000 | 0.11 | 0.03 | |||||
125I-Cmpd 1/Mn2+ | 2.5 | 6.3 | 13.0 | 0% Inh @ 1 mM | 3.5 | 0.22 | |||||
125I-Cmpd 1/Ca2+ Mg2+
|
2.3
|
5.0
|
29.0
|
0% Inh @ 1 mM
|
58.0
|
N.D.
|
N.D., not determined.