Biologically Active Small Molecules

An antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM) used, alone or in combination therapy, in the treatment of pulmonary arterial hypertension.

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.

A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 0.025 nM) inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC₅₀s = 6.5 and 30 &microM, respectively).

A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 0.025 nM) inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC₅₀s = 6.5 and 30 &microM, respectively).

A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 0.025 nM) inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC₅₀s = 6.5 and 30 &microM, respectively).

A linear imidazoquinazoline that potently and selectively inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 8 pM).

A linear imidazoquinazoline that potently and selectively inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 8 pM).

A linear imidazoquinazoline that potently and selectively inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 8 pM).

A bpV compound that selectively inhibits PTEN (IC₅₀ = 14 nM) also inhibits the vascular endothelial PTP, PTP-&beta (IC₅₀ = 4.9 &muM), and PTP-1&betaB (IC₅₀ = 25.3 &muM) with reduced potency.