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

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

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

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

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

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

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

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, 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 efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator with Ki of 0.9 nM, IC50 of 2.5 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 P2Y1 receptor agonist with EC50 of 1.2 nM.

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

A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 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 EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.

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 beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.9 nM in Ca2+ flux assay.

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

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 and orally active antagonist of CB2 receptor with Ki of 0.6 nM.

A highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM).

A highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays.