Respiratory Research

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

From: Dual inhibition of α_vβ₆ and α_vβ₁ reduces fibrogenesis in lung tissue explants from patients with IPF

Compound A (α_vβ₁ inhibitor)			PLN-74809 (dual α_vβ₆/α_vβ₁)
Integrin	Ligand binding IC₅₀ (nM)	Fold selectivity (vs α_vβ₁)	Integrin	Ligand binding IC₅₀ (nM)	Fold selectivity (vs α_vβ₆)
α_vβ₁	2.3	1×	α_vβ₆	5.7	1×
α_vβ₆	49.8	22×	α_vβ₁	3.4	0.6×
α_vβ₃	116.4	51×	α_vβ₃	> 10,000	> 1754×
α_vβ₅	504	221×	α_vβ₅	6989	1226×
α_vβ₈	2933	1286×	α_vβ₈	2539	445×

Integrin	TGF-β activation IC₅₀ (nM)	Fold selectivity (vs α_vβ₁)	Integrin	TGF-β activation IC₅₀ (nM)	Fold selectivity (vs α_vβ₆)
α_vβ₁	7.9	1×	α_vβ₆	29.8	1×
α_vβ₆	6047	765×	α_vβ₁	19.2	0.6×

CWHM-12 (multi-α_v inhibitor)			GSK3008348 (multi-α_v inhibitor)
Integrin	Ligand binding IC₅₀ (nM)	Fold selectivity (vs α_vβ₁)	Integrin	Ligand binding IC₅₀ (nM)	Fold selectivity (vs α_vβ₆)
α_vβ₁	1.3	1×	α_vβ₆	3.4	1×
α_vβ₆	6.1	4.7×	α_vβ₁	4.0	1.2×
α_vβ₃	0.7	0.5×	α_vβ₃	299	89×
α_vβ₅	5.3	4.1×	α_vβ₅	23.5	7.0×
α_vβ₈	7.3	5.6×	α_vβ₈	6.8	2.0×

Integrin	TGF-β activation IC₅₀ (nM)	Fold selectivity (vs α_vβ₁)	Integrin	TGF-β activation IC₅₀ (nM)	Fold selectivity (vs α_vβ₆)
α_vβ₁	2	1×	α_vβ₆	4.7	1×
α_vβ₆	318.0	159×	α_vβ₁	17.4	3.7×

IC₅₀: 50% inhibitory concentration; TGF-β: Transforming growth factor-β

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