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Table 1 Ligand-binding assay IC50 and TGF-β activation assay IC50 for small molecule integrin inhibitors

From: Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF

Compound A (αvβ1 inhibitor) PLN-74809 (dual αvβ6vβ1)
Integrin Ligand binding IC50 (nM) Fold selectivity (vs αvβ1) Integrin Ligand binding IC50 (nM) Fold selectivity (vs αvβ6)
αvβ1 2.3 αvβ6 5.7
αvβ6 49.8 22× αvβ1 3.4 0.6×
αvβ3 116.4 51× αvβ3 > 10,000 > 1754×
αvβ5 504 221× αvβ5 6989 1226×
αvβ8 2933 1286× αvβ8 2539 445×
Integrin TGF-β activation IC50 (nM) Fold selectivity (vs αvβ1) Integrin TGF-β activation IC50 (nM) Fold selectivity (vs αvβ6)
αvβ1 7.9 αvβ6 29.8
αvβ6 6047 765× αvβ1 19.2 0.6×
CWHM-12 (multi-αv inhibitor) GSK3008348 (multi-αv inhibitor)
Integrin Ligand binding IC50 (nM) Fold selectivity (vs αvβ1) Integrin Ligand binding IC50 (nM) Fold selectivity (vs αvβ6)
αvβ1 1.3 αvβ6 3.4
αvβ6 6.1 4.7× αvβ1 4.0 1.2×
αvβ3 0.7 0.5× αvβ3 299 89×
αvβ5 5.3 4.1× αvβ5 23.5 7.0×
αvβ8 7.3 5.6× αvβ8 6.8 2.0×
Integrin TGF-β activation IC50 (nM) Fold selectivity (vs αvβ1) Integrin TGF-β activation IC50 (nM) Fold selectivity (vs αvβ6)
αvβ1 2 αvβ6 4.7
αvβ6 318.0 159× αvβ1 17.4 3.7×
  1. IC50: 50% inhibitory concentration; TGF-β: Transforming growth factor-β