Biologically Active Small Molecules

A double prodrug that undergoes in vivo hydrolytic cleavage to produce dabigatran, a potent thrombin inhibitor (Ki = 4.5 nM) shows antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action.

A double prodrug that undergoes in vivo hydrolytic cleavage to produce dabigatran, a potent thrombin inhibitor (Ki = 4.5 nM) shows antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action.

Molecular Formula: C₂₄H₂₈D₁₃N₇O₅ Formula Weight: 640.8

Molecular Formula: C₂₄H₂₈D₁₃N₇O₅ Formula Weight: 640.8

A potent thrombin inhibitor (Ki = 4.5 nM) also inhibits trypsin (Ki = 50.3 nM), but only weakly inhibits other serine proteases has poor bioavailability after oral administration.

A potent thrombin inhibitor (Ki = 4.5 nM) also inhibits trypsin (Ki = 50.3 nM), but only weakly inhibits other serine proteases has poor bioavailability after oral administration.

A potent thrombin inhibitor (Ki = 4.5 nM) also inhibits trypsin (Ki = 50.3 nM), but only weakly inhibits other serine proteases has poor bioavailability after oral administration.

A potent thrombin inhibitor (Ki = 4.5 nM) also inhibits trypsin (Ki = 50.3 nM), but only weakly inhibits other serine proteases has poor bioavailability after oral administration.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.