A highly potent, selective platelet activating factor (PAF) inhibitor with IC50 of 75 and 170 nM for aggregation inhibition of rabbit and human platelets induced by PAF.

A highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator with Ki of 0.9 nM, IC50 of 2.5 nM.

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

A highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.

A highly potent, selective, orally available Src family kinase inhibitor with IC50 of <0.5 nM, <0.5 nM and for Src, Yes and Fyn kinases respectively, >950-fold selectivity for Src over ABL.

A highly potent, selective, second generation prostaglandin E2 subtype 4 receptor (EP4) antagonist with Ki of 0.56 nM.

A highly potent, specific and cell permeant inhibitor of human proline endopeptidase (PE) with Ki of 1 nM.

A highly potent, subtype-selective agonist of 5-HT2C receptor with Ki of 10.5 nM, >20-fold selectivity over 5-HT2A and 5-HT2B receptor subtypes (IC50=212 and 485 nM, respectively).

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly selective and potent GRK2 (G protein-coupled receptor kinase 2) inhibitor with IC50 of 130 nM.

A highly selective CYP17A1 (17,20-lyase) inhibitor with IC50 of 17 nM for human 17,20-lyase.

A highly selective inhibitor of the FMN riboswitch that controls expression of de novo riboflavin (Vitamin B2) biosynthesis in Escherichia coli.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-peptide agonist of the δ-opioid receptor (δ-OR) with IC50/Ki of 2.73/0.18 nM.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, small molecule inhibitor of the miRNA regulatory complex RISC subunit SND1.

A highly specific myosin II ATPase inhibitor.