Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.

BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.

ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.

Risuteganib hydrochloride is a synthetic RGD (arginyl-glycyl-aspartic acid)-class peptide. Risuteganib hydrochloride is an anti-integrin that downregulates oxidative stress and restores homeostasis, and targets three integrin receptors that are implicated in dry age-related macular degeneration (AMD) in order to restore homeostasis in the retina.

α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.

BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.

αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.

Zaurategrast(CDP-323) is an oral α4-integrin inhibitor.

Valategrast (R411), a small molecule antagonist of α4β1 integrin, represents a potential therapy for asthma

DS-70 (α4 integrin inhibitor DS-70) is a novel potent α/β- peptidomimetic antagonist of α4 integrin, binds to integrin α4β1 with nanomolar affinity.

BIO1211 (BIO-1211) is a potent, highly specific integrin α4β1 (VLA-4) inhibitor with Kd/IC50 of 20 pM/4 nM for the activated form of α4β1.