A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) partial agonist with EC50 of 17 nM, >1,000-fold selectivity over human adrenergic α2A receptor.

A highly potent, selective and time-dependent Cdc7 kinase inhibitor with IC50 of 0.7 nM with slow dissociation property, with 200-fold and >14,000-fold selectivity over CDK2 and ROCK1, respectively.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.2 nM in Ca2+ flux assay.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.9 nM in Ca2+ flux assay.

A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay.

A highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.

A highly potent, selective imidazoline I2 receptor agonist with Ki of 9.8 nM, enhances supraspinal morphine analgesia in mice..

A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM.

A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A highly potent, selective P2Y1 receptor agonist with EC50 of 1.2 nM.

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, brain-penetrating and orally active phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 0.61 nM.

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 active renin inhibitor with IC50 of 2.1 nM in hPRA assay.

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, orally bioavailable HCV NS5B polymerase inhibitor with IC50 of 9, 4, and 18 nM for GT1a, GT1b, and GT1b-C316N mutant in HCV replicon assay, respectively.

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.