iRGD peptide (sequence: CRGDKGPDC) is a 9-amino acid cyclic peptide, and a molecular mimicry agent that was originally identified in an in vivo screening of phage display libraries in tumor-bearing mice.

THI-0019 (THI0019) is a novel and potent integrin α4β1 (VLA-4) agonist (EC50 in the range of 1-2 μM).

Firategrast (formerly SB683699; T0047; SB-683699; T-0047) is a novel, potent and orally bioavailable alpha4 beta1/alpha4 beta7 (α4β1/α4β7) integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).

Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.

Leukadherin-1, formerly known as LA1, is a novel and specific agonist of Complement receptor 3 (CR3) and the leukocyte surface integrin CD11b/CD18 that enhances leukocyte adhesion to ligands and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites.

SB273005 (SB 273005; SB-273005) is a novel and potent integrin inhibitor with potential usefulness in bone resorption, osteoporosis and arthritis.

TR-14035 is a novel, dual antagonist of alpha4beta7 integrin with IC50 of 7 nM and alpha4beta1 integrin with IC50 of 87 nM.

Tirofiban (formerly known as L-700462; MK-383; L700462; MK383; Aggrastat) is a novel non-peptide antagonist of glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) that has been approved for use as an antiplatelet drug.

OSU-T315 (ILK-IN-1) is a novel, potent and specific small molecule inhibitor of Integrin-linked kinase (ILK) with an IC50 of 0.6 μM, suppressing cancer cell proliferation in vitro and in vivo and inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain).

A-286982 is a potent inhibitor of the LFA-1/ICAM-1 interaction with IC50 of 44 nM in an LFA-1/ICAM-1 binding assay.